Mats Larhed
Professor at Institutionen för läkemedelskemi; Preparativ läkemedelskemi
- Mobile phone:
- +46 70 493 53 83
- E-mail:
- mats.larhed@ilk.uu.se
- Visiting address:
- Uppsala Biomedicinska Centrum, BMC, Husarg. 3
- Postal address:
- Box 574
751 23 UPPSALA
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Short presentation
Mats Larhed was born in Västerås, Sweden, on August 21, 1964. He graduated in 1991 with a Master of Science in Pharmacy. His doctoral studies in Organic Pharmaceutical Chemistry were accomplished in 1997. He became Senior Lecturer in 2001, was appointed full Professor in Combinatorial Chemistry 2007, before being appointed at Uppsala University as Professor in Medicinal Chemistry in 2015. He was elected as Vice-Rector for Medicine and Pharmacy in 2020. For full CV, see link below:
Keywords
- angiotensin
- antibiotics
- flow chemistry
- irap
- microwave chemistry
- palladium
- pulmonary fibrosis
Biography
Mats Larhed is Professor in Medicinal Chemistry and holds at present the position as Vice-Rector for the Disciplinary Domain of Medicine and Pharmacy at Uppsala University.
Larhed is engaged in the development of the Beijer laboratory for drug discovery. He is also member of the national SciLifeLab Board,
Larhed is interested in the development of career paths at universities and he was the Chair of the Uppsala University working group on career paths and was responsible for the approved Uppsala Universities Charter & Code Human Resources Strategy for Researchers (HRS4R) application. He has served as chair for quality assurance evaluations of the Swedish University of Agricultural Sciences (SLU) and of the University of Borås.
Larhed is member of The Royal Society of Sciences in Uppsala, The Society of Arts and Sciences of Uppsala and The Royal Swedish Academy of Engineering Sciences (IVA).
Mats Larheds teaching activities have been directed toward students in pharmacy, chemical engineering and biomedicine. He early developed web-based examinations and lectures for his chemistry courses. His web lectures have been viewed > 30 000 times. He has overseen 22 PhD students to a final doctorate as the main supervisor and is presently supervising one PhD student and two PostDoc students.
Larheds main research interests are: I) the discovery and development of new pharmaceutical agents for treatment of pulmonary fibrosis (IPF) and other inflammatory diseases, II) development of new chemical methodologies of importance for drug discovery.
Larhed has received a number of grants from for example the Knut and Alice Wallenberg Foundation, the Swedish Research Council and the European Commission Framework Programs as well as a couple of prestigious awards, including The Holmquist Prize. He has published more than 220 scientific articles and a number of approved patents.
Publications
Selection of publications
- Angiotensin II AT2 receptor ligands with phenylthiazole scaffolds (2022)
- 2-Alkyl substituted benzimidazoles as a new class of selective AT2 receptor ligands (2022)
- N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands (2021)
- Regio- and Stereoselective Synthesis of Allylic Spiroethers (Spirobenzofuranes) via an Intramolecular Mizoroki-Heck Reaction (2020)
- Synthesis, Evaluation and Proposed Binding Pose of Substituted Spiro-Oxindole Dihydroquinazolinones as IRAP Inhibitors (2020)
- From Angiotensin IV to Small Peptidemimetics Inhibiting Insulin-Regulated Aminopeptidase (2020)
- Regio- and Stereoselective Synthesis of Spirooxindoles via Mizoroki-Heck Coupling of Aryl Iodides (2019)
- A Series of Analogues to the AT2R Prototype Antagonist C38 Allow Fine Tuning of the Previously Reported Antagonist Binding Mode (2019)
- Palladium-Catalyzed Molybdenum Hexacarbonyl-Mediated Gas-Free Carbonylative Reactions (2019)
- Selective Synthesis of Spirooxindoles by an Intramolecular Heck-Mizoroki Reaction (2017)
- Identification of Drug-Like Inhibitors of Insulin-Regulated Aminopeptidase Through Small-Molecule Screening (2016)
- NONPEPTIDE AT2 RECEPTOR AGONISTS (2016)
- Synthesis of 4-Quinolones via a Carbonylative Sonogashira Cross-Coupling Using Molybdenum Hexacarbonyl as a CO Source (2015)
- Synthesis of P1 '-Functionalized Macrocyclic Transition-State Mimicking HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol (2014)
- Aspartic protease inhibitors containing tertiary alcohol transition-state mimics (2014)
- Microwave-assisted synthesis of small molecules targeting the infectious diseases tuberculosis, HIV/AIDS, malaria and hepatitis C (2012)
- Aminocarbonylations Employing Mo(CO)(6) and a Bridged Two-Vial System (2012)
- Transmetallation Versus β-Hydride Elimination (2012)
- Synthesis, X-ray Analysis, and Biological Evaluation of a New Class of Stereopure Lactam-Based HIV-1 Protease Inhibitors (2012)
- Evaluation of a Nonresonant Microwave Applicator for Continuous-Flow Chemistry Applications (2012)
Recent publications
- Inhibition of Insulin-Regulated Aminopeptidase by Imidazo[1,5-α]pyridines; Synthesis and Evaluation (2024)
- The decanoate esters of nandrolone, testosterone, and trenbolone induce steroid specific memory impairment and somatic effects in the male rat (2024)
- Two-chamber Aminocarbonylation of Aryl Bromides and Triflates Using Amino Acids as Nucleophiles (2023)
- Angiotensin II AT2 receptor ligands with phenylthiazole scaffolds (2022)
- Diastereoselective Synthesis of N-Methylspiroindolines by Intramolecular Mizoroki–Heck Annulations (2022)
All publications
Articles
- Inhibition of Insulin-Regulated Aminopeptidase by Imidazo[1,5-α]pyridines; Synthesis and Evaluation (2024)
- The decanoate esters of nandrolone, testosterone, and trenbolone induce steroid specific memory impairment and somatic effects in the male rat (2024)
- Two-chamber Aminocarbonylation of Aryl Bromides and Triflates Using Amino Acids as Nucleophiles (2023)
- Angiotensin II AT2 receptor ligands with phenylthiazole scaffolds (2022)
- Diastereoselective Synthesis of N-Methylspiroindolines by Intramolecular Mizoroki–Heck Annulations (2022)
- Synthesis and in vitro biological evaluation of quinolinyl pyrimidines targeting type II NADH-dehydrogenase (NDH-2) (2022)
- 2-Alkyl substituted benzimidazoles as a new class of selective AT2 receptor ligands (2022)
- Hydrogen Peroxide Induced Toxicity Is Reversed by the Macrocyclic IRAP-Inhibitor HA08 in Primary Hippocampal Cell Cultures (2022)
- 18F-Radiolabeling and Preliminary Evaluation of a HSP90 ligand (2021)
- N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands (2021)
- Regio- and Stereoselective Synthesis of Allylic Spiroethers (Spirobenzofuranes) via an Intramolecular Mizoroki-Heck Reaction (2020)
- Macrocyclic Peptidomimetics as Inhibitors of Insulin-Regulated Aminopeptidase (IRAP) (2020)
- Synthesis, Evaluation and Proposed Binding Pose of Substituted Spiro-Oxindole Dihydroquinazolinones as IRAP Inhibitors (2020)
- From Angiotensin IV to Small Peptidemimetics Inhibiting Insulin-Regulated Aminopeptidase (2020)
- Direct stimulation of angiotensin II type 2 receptor reduces nitric oxide production in lipopolysaccharide treated mouse macrophages (2020)
- Heterodimeric Radiotracer Targeting PSMA and GRPR for Imaging of Prostate Cancer-Optimization of the Affinity towards PSMA by Linker Modification in Murine Model (2020)
- Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor (2020)
- Synthesis and Preclinical Evaluation of Radio-Iodinated GRPR/PSMA Bispecific Heterodimers for the Theranostics Application in Prostate Cancer (2019)
- Regio- and Stereoselective Synthesis of Spirooxindoles via Mizoroki-Heck Coupling of Aryl Iodides (2019)
- Synthesis and preclinical evaluation of the CRTH2 antagonist [11C]MK-7246 as a novel PET tracer and potential surrogate marker for pancreatic beta-cell mass (2019)
- A Series of Analogues to the AT2R Prototype Antagonist C38 Allow Fine Tuning of the Previously Reported Antagonist Binding Mode (2019)
- Trastuzumab cotreatment improves survival of mice with PC-3 prostate cancer xenografts treated with the GRPR antagonist 177Lu-DOTAGA-PEG2-RM26 (2019)
- Bispecific GRPR-antagonistic anti-PSMA/GRPR heterodimer for PET and SPECT diagnostic imaging of prostate cancer (2019)
- Palladium-Catalyzed Molybdenum Hexacarbonyl-Mediated Gas-Free Carbonylative Reactions (2019)
- Structural Basis of Inhibition of Human Insulin-Regulated Aminopeptidase (IRAP) by Aryl Sulfonamides (2018)
- A convenient transesterification method for synthesis of AT2 receptor ligands with improved stability in human liver microsomes (2018)
- Continuous Flow Synthesis under High-Temperature/High-Pressure Conditions Using a Resistively Heated Flow Reactor (2017)
- Synthesis of 11C-Labelled Ureas by Palladium(II)-Mediated Oxidative Carbonylation (2017)
- Lignin depolymerization to monophenolic compounds in a flow-through system (2017)
- High Contrast PET Imaging of GRPR Expression in Prostate Cancer Using Cobalt-Labeled Bombesin Antagonist RM26 (2017)
- Synthesis and In Vitro Evaluation of 5-Substituted Benzovesamicol Analogs containing N-Substituted Amides as Potential Positron Emission Tomography Tracers for the Vesicular Acetylcholine Transporter (2017)
- Selective Synthesis of Spirooxindoles by an Intramolecular Heck-Mizoroki Reaction (2017)
- Route to 3-Amidino Indoles via Pd(II)-Catalyzed C-H Bond Activation (2017)
- Regio- and Stereoselective Synthesis of Functionalized Cyclopentene Derivatives via Mizoroki-Heck Reactions. (2017)
- Synthesis of 4H-Benzo[e][1,3]oxazin-4-ones by a Carbonylation-Cyclization Domino Reaction of ortho-Halophenols and Cyanamide (2017)
- Palladium(0)-Catalyzed Carbonylative One-Pot Synthesis of N-Acylguanidines (2017)
- Binding to and Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Macrocyclic Disulfides Enhances Spine Density (2016)
- Aryl Sulfonamide Inhibitors of Insulin-Regulated Aminopeptidase Enhance Spine Density in Primary Hippocampal Neuron Cultures (2016)
- Identification of Drug-Like Inhibitors of Insulin-Regulated Aminopeptidase Through Small-Molecule Screening (2016)
- Rapid and straightforward transesterification of sulfonyl carbamates (2016)
- Microwave Promoted Transcarbamylation Reaction of Sulfonylcarbamates under Continuous-Flow Conditions (2016)
- NONPEPTIDE AT2 RECEPTOR AGONISTS (2016)
- Selection of optimal chelator improves the contrast of GRPR imaging using bombesin analogue RM26. (2016)
- Microwave Heated Continuous Flow Palladium(II)-Catalyzed Desulfitative Synthesis of Aryl Ketones (2016)
- Synthesis of 11C-labelled Sulfonyl Carbamates via a Multicomponent Reaction Employing Sulfonyl Azides, Alcohols and [11C]CO (2016)
- Synthesis of C-11-labeled Sulfonyl Carbamates through a Multicomponent Reaction Employing Sulfonyl Azides, Alcohols, and [C-11]CO (2016)
- Palladium-Catalyzed Carbonylation of Aryl Iodides with Sulfinamides (2015)
- Development of radiocobalt-labeled GRPR antagonist NOTA-PEG2-RM26. (2015)
- Rapid and Efficient Conversion of (CO2)-C-11 to (CO)-C-11 through Silacarboxylic Acids (2015)
- Chemical Conversion of (CO2)-C-11 to (CO)-C-11 via Silacarboxylic Acids (2015)
- Influence of chelators on targeting properties of In-111 and Ga-68 labeled GRPR antagonist (2015)
- 3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1 (2015)
- N-Substituted pyrazole-3-carboxamides as inhibitors of human 15-lipoxygenase (2015)
- Optimization and Evaluation of 5-Styryl-Oxathiazol-2-one Mycobacterium tuberculosis Proteasome Inhibitors as Potential Antitubercular Agents (2015)
- Site-Specific Radioiodination of HER2-Targeting Affibody Molecules using 4-Iodophenethylmaleimide Decreases Renal Uptake of Radioactivity (2015)
- Virtual Screening for Transition State Analogue Inhibitors of IRAP Based on Quantum Mechanically Derived Reaction Coordinates (2015)
- The effect of macrocyclic chelators on the targeting properties of the 68Ga-labeled gastrin releasing peptide receptor antagonist PEG2-RM26 (2015)
- Synthesis of enantiopure angiotensin II type 2 receptor [AT(2)R] antagonist EMA401 (2015)
- Synthesis of 4-Quinolones via a Carbonylative Sonogashira Cross-Coupling Using Molybdenum Hexacarbonyl as a CO Source (2015)
- An Improved Palladium(II)-Catalyzed Method for the Synthesis of Aryl Ketones from Aryl Carboxylic Acids and Organonitriles (2014)
- N-Aryl Isoleucine Derivatives as Angiotensin II AT(2) Receptor Ligands (2014)
- Synthesis and Labelling of a Piperazine-Based Library of 11C-Labeled Ligands for Imaging of the Vesicular Acetylcholine Transporter (2014)
- Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides (2014)
- Syntheses of new tuberculosis inhibitors promoted by microwave irradiation (2014)
- Synthesis of P1 '-Functionalized Macrocyclic Transition-State Mimicking HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol (2014)
- Nonresonant microwave heated continuous flow synthesis in medicinal chemistry (2014)
- Microwave Heated Flow Synthesis of Spiro-oxindole Dihydroquinazolinone Based IRAP Inhibitors (2014)
- Palladium(II)-Catalyzed Decarboxylative Heck Arylations of Acyclic Electron-Rich Olefins with Internal Selectivity (2014)
- Achiral Pyrazinone-Based Inhibitors of the Hepatitis C Virus NS3 Protease and Drug-Resistant Variants with Elongated Substituents Directed Toward the S2 Pocket (2014)
- Safe Palladium-Catalyzed Cross-Couplings with Microwave Heating Using Continuous-Flow Silicon Carbide Reactors (2014)
- Continuous flow chemistry utilizing silicon carbide (SiC) reactors (2014)
- Influence of chelators on biodistribution and targeting properties of GRPR antagonist (2014)
- Aspartic protease inhibitors containing tertiary alcohol transition-state mimics (2014)
- C-11-Labeling of a potent hydroxyethylamine BACE-1 inhibitor and evaluation in vitro and in vivo (2014)
- 11C-Labeling of a Potent Hydroxyethylamine BACE-1 Inhibitor and Evaluation in vitro and in vivo (2014)
- Continuous flow chemistry with a non-resonant microwave applicator (2014)
- Palladium(II) catalyzed desulfitative coupling reactions of sodium aryl sulfinates and nitriles (2014)
- Palladium(II)-Catalyzed Desulfitative Synthesis of Aryl Ketones from Sodium Arylsulfinates and Nitriles (2014)
- The Effect of Mini-PEG-Based Spacer Length on Binding and Pharmacokinetic Properties of a Ga-68-Labeled NOTA-Conjugated Antagonistic Analog of Bombesin (2014)
- Synthesis and evaluation of isoleucine derived angiotensin II AT(2) receptor ligands (2014)
- Synthesis and biological evaluation of a piperazine-based library of C-11-Labeled PET tracers for imaging of the vesicular acetylcholine transporter (2013)
- DXR Inhibition by Potent Mono- and Disubstituted Fosmidomycin Analogues (2013)
- Design and Synthesis of P1-P3 Macrocyclic Tertiary-Alcohol-Comprising HIV-1 Protease Inhibitors (2013)
- Palladium-Catalyzed Carbonylative Synthesis of N-Cyanobenzamides from Aryl Iodides/Bromides and Cyanamide (2013)
- Diarylated Ethanones from Mo(CO)(6)-Mediated and Microwave-Assisted Palladium-Catalysed Carbonylative Negishi Cross-Couplings (2013)
- Temperature measurements with two different IR sensors in a continuous-flow microwave heated system (2013)
- Decarboxylative Palladium(II)-Catalyzed Synthesis of Aryl Amidines from Aryl Carboxylic Acids (2013)
- Aminocarbonylation of 4-Iodo-1H-imidazoles with an Amino Acid Amide Nucleophile (2013)
- Synthesis of antimalarial compounds fosmidomycin and FR900098 through N- or P-alkylation reactions (2013)
- Theoretical and Experimental Investigation of Palladium(II)-Catalyzed Decarboxylative Addition of Arenecarboxylic Acid to Nitrile (2013)
- Optimizing Solubility and Permeability of a Biopharmaceutics Classification System (BCS) Class 4 Antibiotic Drug Using Lipophilic Fragments Disturbing the Crystal Lattice (2013)
- Synthesis and Characterization of a High-Affinity NOTA-Conjugated Bombesin Antagonist for GRPR-Targeted Tumor Imaging (2013)
- GRPR antagonist NOTA-P2-RM26 labeled with fluorine-18 (2013)
- In Vitro and In Vivo Evaluation of a F-18-Labeled High Affinity NOTA Conjugated Bombesin Antagonist as a PET Ligand for GRPR-Targeted Tumor Imaging (2013)
- One-Pot, Two-Step, Microwave-Assisted Palladium-Catalyzed Conversion of Aryl Alcohols to Aryl Fluorides via Aryl Nonaflates (2013)
- (AlF)-F-18-labelling of NOTA-P2-RM26 and its evaluation as a PET ligand for GRPR/BB2 (2013)
- Synthesis of functionalized furopyrazines as restricted dipeptidomimetics (2012)
- A non-resonant microwave applicator fully dedicated to continuous flow chemistry (2012)
- Trisubstituted Imidazoles as Mycobacterium tuberculosis Glutamine Synthetase Inhibitors (2012)
- Microwave-assisted synthesis of small molecules targeting the infectious diseases tuberculosis, HIV/AIDS, malaria and hepatitis C (2012)
- Aminocarbonylations Employing Mo(CO)(6) and a Bridged Two-Vial System (2012)
- Synthesis, biological evaluation and X-ray crystallographic studies of imidazo[1,2-a]-pyridine based Mycobacterium tuberculosis glutamine synthetase inhibitors (2012)
- Molybdenum Hexacarbonyl Mediated CO Gas-Free Carbonylative Reactions (2012)
- Transmetallation Versus β-Hydride Elimination (2012)
- Site-specific radioiodination of HER2-targeting affibody molecules using iodophenetylmaleimide decreases renal uptake of radioactivity (2012)
- Oxidative Heck Reactions Using Aryltrifluoroborates and Aryl N-Methyliminodiacetic Acid (MIDA) Boronates (2012)
- Direct Palladium(II)-Catalyzed Synthesis of Arylamidines from Aryltrifluoroborates (2012)
- Development of Stereocontrolled Palladium(II)-Catalyzed Domino Heck/Suzuki β, α-Diarylation Reactions with Chelating Vinyl Ethers and Arylboronic Acids (2012)
- Synthesis and characterization of a high affinity NOTA-conjugated bombesin antagonist for GRPR-targeted tumor imaging (2012)
- Synthesis, X-ray Analysis, and Biological Evaluation of a New Class of Stereopure Lactam-Based HIV-1 Protease Inhibitors (2012)
- Evaluation of a Nonresonant Microwave Applicator for Continuous-Flow Chemistry Applications (2012)
- Design, Synthesis, and X-ray Crystallographic Studies of alpha-Aryl Substituted Fosmidomycin Analogues as Inhibitors of Mycobacterium tuberculosis 1-Deoxy-D-xylulose 5-Phosphate Reductoisomerase (2011)
- Substitution of the phosphonic acid and hydroxamic acid functionalities of the DXR inhibitor FR900098 (2011)
- Microwave-Assisted Palladium(II)-Catalyzed Synthesis of Aryl Ketones from Aryl Sulfinates and Direct ESI-MS Studies Thereof (2011)
- Structural Features Determining the Intestinal Epithelial Permeability and Efflux of Novel HIV-1 Protease Inhibitors (2011)
- Synthesis of Functionalized Cinnamaldehyde Derivatives by an Oxidative Heck Reaction and Their Use as Starting Materials for Preparation of Mycobacterium tuberculosis 1-Deoxy-D-xylulose-5-phosphate Reductoisomerase Inhibitors (2011)
- Richard F. Heck (2011)
- Non-peptide AT2-receptor agonists (2011)
- Microwave-Assisted Synthesis of Weinreb and MAP Aryl Amides via Pd-Catalyzed Heck Aminocarbonylation Using Mo(CO)(6) or W(CO)(6) (2011)
- Investigation of alpha-phenylnorstatine and alpha-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors (2011)
- Chelation-Mediated Palladium(II)-Catalyzed Domino Heck-Mizoroki/Suzuki-Miyaura Reactions Using Arylboronic Acids (2011)
- Hiv-1 Protease Inhibitors with a Tertiary Alcohol Containing a Transition-State Mimic and Various P2/P1´ Substituents (2011)
- Synthesis of a small library of non-symmetric cyclic sulfamide HIV-1 protease inhibitors (2010)
- Hepatitis C protease inhibitors based on 2(1H)-pyrazinones (2010)
- Synthesis of aryl ketones by palladium(II)-catalyzed decarboxylative addition of benzoic acids to nitriles (2010)
- HIV-1 Protease Inhibitors with a Transition-State Mimic Comprising a Tertiary Alcohol (2010)
- Continuous Flow Palladium(II) (2010)
- Synthesis and evaluation of a 11C-labelled angiotensin II AT2 receptor ligand (2010)
- Discovery of Achiral Inhibitors of the Hepatitis C Virus NS3 Protease based on 2(1H)-pyrazinones (2010)
- Microwave-promoted palladium(II)-catalyzed C-P bond formation by using arylboronic acids or aryltrifluoroborates. (2009)
- A straightforward microwave method for rapid synthesis of N-1, C-6 functionalized 3,5-dichloro-2(1H)-pyrazinones (2009)
- Aminocarbonylations of Alkenyl Phosphates, Chlorides, Bromides and Triflates with Mo(CO)6 as a Solid CO source (2009)
- Microwave-assisted palladium(II)-catalyzed Heck reactions (2009)
- Synthesis of styrenes by palladium(II)-catalyzed vinylation of arylboronic acids and aryltrifluoroborates by using vinyl acetate (2009)
- Structural basis for the inhibition of Mycobacterium tuberculosis glutamine synthetase by novel ATP-competitive inhibitors (2009)
- Functionalized 3-amino-imidazo[1,2-a]pyridines (2009)
- α-Substituted Norstatines as the Transistion-State Mimic in Inhibitors of Multiple Digestive Vacuole Malaria Aspartic Proteases (2009)
- Synthesis and evaluation of a new class of tertiary alcohol based BACE-1 inhibitors (2009)
- Palladium(II)-catalyzed coupling reactions with a chelating vinyl ether and arylboronic acids (2009)
- Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic (2009)
- Microwave-assisted, Mo(CO)(6)-mediated, palladium-catalyzed amino-carbonylation of aryl halides using allylamine (2008)
- High Stereoselectivity in Chelation-Controlled Intermolecular Heck Reactions with Aryl Chlorides, Vinyl Chlorides and Vinyl Triflates (2008)
- Enantiopure 2-Aryl-2-Methyl Cyclopentanones by an Asymmetric Chelation-Controlled Heck Reaction Using Aryl Bromides (2008)
- Evaluation of the amino acid binding site of Mycobacterium tuberculosis glutamine synthetase for drug discovery (2008)
- Microwave-promoted aminocarbonylation of aryl triflates using Mo(CO)(6) as a solid CO source (2008)
- Fast, acid-free, and selective lactamization of lactones in ionic liquids (2008)
- Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors (2008)
- A mechanistic study on modern palladium catalyst precursors as new gateways to Pd(0) in cationic Heck reactions (2008)
- Stereoselective Heck arylation of a functionalized cyclopentenyl ether using (S)-N-methyl-pyrrolidine as the stereochemical controller (2008)
- Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic (2008)
- Highly regioselective internal heck arylation of hydroxyalkyl vinyl ethers by aryl halides in water (2007)
- Synthesis of a new class of druglike angiotensin II C-terminal mimics with affinity for the AT2 receptor (2007)
- Microwave-enhanced alpha-arylation of a protected glycine in water (2007)
- Controlled microwave heating as an enabling technology (2007)
- Efficient palladium(II) catalysis under air. Base-free oxidative heck reactions at room temperature or with microwave heating (2007)
- Microwave-Enhanced Copper-Catalyzed N-Arylation of Free and Protected Amino Acids in Water (2007)
- Microwave-accelerated spiro-cyclizations of o-halobenzyl cyclohexenyl ethers by palladium(0) catalysis (2007)
- Stereoselective Synthesis of 3-Aminoindan-1-ones and Subsequent Incorporation into HIV-1 Protease Inhibitors (2006)
- Selective Terminal Heck Arylation of Vinyl Ethers with Aryl Chlorides: A Combined Experimental-Computational Approach Including Synthesis of Betaxolol (2006)
- Selective terminal heck arylation of vinyl ethers with aryl chlorides (2006)
- Microwave-Accelerated Synthesis of P1´-Extended HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol in the Transition-State Mimicking Scaffold (2006)
- Variations of the P2 Group in HIV-1 Protease Inhibitors Containing a Tertiary Alcohol in the Transition-State Mimicking Scaffold (2006)
- Microwave-accelerated synthesis of P1'-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold (2006)
- Open-air oxidative Heck reactions at room temperature (2006)
- ESI-MS Detection of Proposed Reaction Intermediates in the Air-Promoted and Ligand-Modulated Oxidative Heck Reaction (2006)
- Fast and selective synthesis of novel cyclic sulfamide HIV-1 purchase inhibitors under controlled microwave heating (2006)
- Microwave-assisted and metal-catalyzed coupling reactions (2006)
- Microwave-accelerated synthesis of protease inhibitors (2006)
- A New Structural Theme in C2-Symmetric HIV-1 Protease Inhibitors: ortho-Substituted P1/P1’ Side Chains (2006)
- Microwave-promoted aminocarbonylation of aryl iodides, aryl bromides and aryl chlorides in water. (2006)
- Microwave-Promoted Aminocarbonylation of Aryl Iodides, Aryl Bromides, and Aryl Chlorides in Water (2006)
- Hydroxylamine as an ammonia equivalent in microwave-enhanced aminocarbonylations (2006)
- Masked 3-Aminoindan-1-ones by a Palladium-Catalyzed Three-Component Annulation Reaction (2005)
- Masked 3-aminoindan-1-ones by a palladium-catalyzed three-component annulation reaction. (2005)
- Super fast cobalt carbonyl-mediated synthesis of ureas compounds (2005)
- Super fast cobalt carbonyl-mediated synthesis of ureas (2005)
- Microwave Irradiation as a High-Speed Toll for Activation of Sluggish Aryl Chlorides in Grignard Reactions (2005)
- All the rave in microwaves. (2005)
- Microwave-promoted aminocarbonylations of aryl chlorides using Mo(CO)(6) as a solid carbon monoxide source. (2005)
- A One-Pot Isomerization-Arylation of 2,3-Epoxycyclohexanone under Controlled Microwave Heating (2005)
- A one-pot isomerization-arylation of 2,3-epoxycyclohexanone under controlled microwave heating. (2005)
- Microwave-Enhanced and Metal-Catalyzed Functionalizations of the 4-Aryl-Dihydropyrimidone Template (2005)
- Microwave-enhanced aminocarbonylations in water. (2005)
- Microwave-enhanced carbonylative generation of indanones and 3-acylaminoindanones. (2005)
- Easy-to-Execute Carbonylations: Microwave Synthesis of Acyl Sulfonamides Using Mo(CO)6 as a Solid Carbon Monoxide Source (2005)
- Easy-to-execute carbonylations (2005)
- The first ligand-modulated oxidative Heck vinylation. Efficient catalysis with molecular oxygen as palladium(0) oxidant. (2004)
- Dioxygen-promoted regioselective oxidative heck arylations of electron-rich olefins with arylboronic acids. (2004)
- Microwave-enhanced medicinal chemistry (2004)
- Direct Microwave Synthesis of N,N'-diacylhydrazines and Boc-protected Hydrazides by in situ Carbonylations under Air (2004)
- Direct microwave synthesis of N,N'-diacylhydrazines and Boc-protected hydrazides by in situ carbonylations under air. (2004)
- An efficient method to perform milliliter-scale PCR utilizing highly controlled microwave thermocycling. (2004)
- An efficient method to perform milliliter-scale PCR utilizing highly controlled microwave thermocycling (2004)
- Terminal Heck vinylations of chelating vinyl ethers. (2004)
- Microwave-Promoted and Chelation-Controlled Double Arylation of Terminal Olefinic Carbon of Vinyl Ethers. (2004)
- Microwave-promoted and chelation-controlled double arylations of terminal olefinic carbon of vinyl ethers. (2004)
- Arylboronic acids as versatile coupling partners in fast microwave promoted oxidative Heck chemistry (2003)
- A rapid microwave protocol for Heck vinylation of aryl chlorides under air. (2003)
- A Rapid Microwave Protocol for Heck Vinylation of Aryl Chlorides under Air (2003)
- Ultrafast Chemistry: Cobalt Carbonyl-Mediated Synthesis of Diaryl Ketones under Microwave Irradiation (2003)
- Microwave-assisted high-speed PCR (2003)
- Rapid palladium-catalyzed synthesis of esters from aryl halides utilizing Mo(CO)6 as a solid carbon monoxide source (2003)
- A New Highly Asymmetric Chelation-Controlled Heck Arylation (2003)
- High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II (2003)
- Increasing Rates and Scope of Reactions (2003)
- Fast Synthesis of Aryl Triflates with Controlled Microwave Heating (2002)
- Protected Indanones by a Heck-Aldol Annulation Reaction (2002)
- Microwave-Assisted Enantioselective Heck Reactions: Expediting High Reaction Speed and Preparative Convenience (2002)
- High-Speed Heck Reactions in Ionic Liquid with Controlled Microwave Heating (2002)
- Highly Regioselective, Sequential and Multiple Palladium-Catalyzed Arylations of Vinyl Ethers Carrying a Coordinating Auxiliary: An Example of a Heck Triarylation Process (2001)
- Aqueous DMF-Potassium Carbonate as a Substitute for Thallium and Silver Additives in the Palladium-Catalyzed Conversion of Aryl Bromides to Acetyl Arenes (2001)
- Highly Selective Palladium-Catalyzed Synthesis of Protected a,ß-Unsaturated Methyl Ketones and 2-Alkoxy-1,3-Butadienes (2000)
- Theoretical Mechanistic Investigation of a Decarboxylative Heck Reaction with an Electron-Rich Olefin and Possible Catalyst Entrapment by the Heck Product
- New Regioselective Heck-Vinylation with Enamides. Synthesis and Investigation of Fluorous Tagged Bidentate Ligands for Fast Separation
Chapters
- Microwave-assisted synthesis of anti-tuberculosis, HIV and hepatitis C agents (2014)
- Microwave-Heated Transition Metal-Catalyzed Coupling Reactions (2012)
- Microwave-Assisted Transition Metal-Catalyzed Asymmetric Synthesis (2011)
- Focus on Regioselectivity and Product Outcome in Organic Synthesis (2009)
- Microwave-accelerated homogenous catalysis in water (2009)
- Accelerated Chemistry (2006)
- Microwave Accelerated Metal Catalysis (2005)
- Palladium-Catalyzed Multiple and Asymmetric Arylations of Vinyl Ethers Carrying Coordinating Nitrogen Auxiliaries (2004)
- Microwave-Assisted Fluorous Chemistry (2004)
- Scope, Mechanism and Other Fundamental Aspects of the Intermolecular Heck Reaction (2002)
- Transition metal-catalysis and microwave flash-heating in organic chemistry (2002)
- Experimental Techniques in Fluorous Synthesis (2000)
Conferences
