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List of works by Karl Barry Sharpless

"Inverse Drug Discovery" Strategy To Identify Proteins That Are Targeted by Latent Electrophiles As Exemplified by Aryl Fluorosulfates

scientific article published on 21 December 2017

"On water": unique reactivity of organic compounds in aqueous suspension

scientific article

.alpha.-Hydroxy ketones in high enantiomeric purity from asymmetric dihydroxylation of enol ethers

2,6-Dichloro-9-thiabicyclo[3.3.1]nonane: Multigram Display of Azide and Cyanide Components on a Versatile Scaffold

scientific article (publication date: 27 March 2006)

2,6-Dichloro-9-thiabicyclo[3.3.1]nonane: a privileged, bivalent scaffold for the display of nucleophilic components

scientific article published in June 2001

A Heck-Matsuda Process for the Synthesis of β-Arylethenesulfonyl Fluorides: Selectively Addressable Bis-electrophiles for SuFEx Click Chemistry

scientific article published on 10 October 2016

A fluorogenic aryl fluorosulfate for intraorganellar transthyretin imaging in living cells and in Caenorhabditis elegans

scientific article published on 8 June 2015

A mechanistic insight leads to a greatly improved osmium-catalyzed asymmetric dihydroxylation process

article

A potent and highly selective inhibitor of human alpha-1,3-fucosyltransferase via click chemistry

scientific article published in August 2003

A stepwise huisgen cycloaddition process: copper(I)-catalyzed regioselective "ligation" of azides and terminal alkynes

scientific article (publication date: 15 July 2002)

A sulfilimine bond identified in collagen IV

scientific article

Addition Reactions with Formation of Carbon–Oxygen Bonds: (ii) Asymmetric Methods of Epoxidation

article

Antiviral stilbene 1,2-diamines prevent initiation of hepatitis C virus RNA replication at the outset of infection

scientific article

Aromatic Sulfonyl Fluorides Covalently Kinetically Stabilize Transthyretin to Prevent Amyloidogenesis while Affording a Fluorescent Conjugate

scientific article

Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr Residue

scientific article published on 18 May 2016

Asymmetric epoxidation provides shortest routes to four chiral epoxy alcohols which are key intermediates in syntheses of methymycin, erythromycin, leukotriene C-1, and disparlure

scientific article published in 1981

Asymmetric induction in the reaction of osmium tetroxide with olefins

scholarly article by Steven G. Hentges & Karl Barry Sharpless published June 1980 in Journal of the American Chemical Society

Automated docking with protein flexibility in the design of femtomolar "click chemistry" inhibitors of acetylcholinesterase

scientific article published on 29 March 2013

Bifluoride-catalysed sulfur(VI) fluoride exchange reaction for the synthesis of polysulfates and polysulfonates

scientific article

Biocompatible SuFEx Click Chemistry: Thionyl Tetrafluoride (SOF4 )-Derived Connective Hubs for Bioconjugation to DNA and Proteins

scientific article published on 08 May 2019

Bioconjugation by copper(I)-catalyzed azide-alkyne [3 + 2] cycloaddition

scientific article published in March 2003

Biological demethylation of 4,4-dimethyl sterols, Evidence for enzymic epimerization of the 4beta-methyl group prior to its oxidative removal

scientific article published on 01 June 1969

Bis(trimethylsilyl) Peroxide Extends the Range of Oxorhenium Catalysts for Olefin Epoxidation

scientific article published in 1997

Bisaryloxime ethers as potent inhibitors of transthyretin amyloid fibril formation

scientific article

Bringing Efficiency to Materials Synthesis: The Philosophy of Click Chemistry

Catalytic Asymmetric Aminohydroxylation(AA) of Olefins

Catalytic Asymmetric Dihydroxylation

Catalytic asymmetric epoxidation and kinetic resolution: modified procedures including in situ derivatization

article

Centrally acting oximes in reactivation of tabun-phosphoramidated AChE.

scientific article

Chemoselective Synthesis of Polysubstituted Pyridines from Heteroaryl Fluorosulfates

scientific article published on 15 March 2016

Chitinase inhibitors: extraction of the active framework from natural argifin and use of in situ click chemistry

scientific article

Click Chemistry-Facilitated Structural Diversification of Nitrothiazoles, Nitrofurans, and Nitropyrroles Enhances Antimicrobial Activity against Giardia lamblia

scientific article

Click Chemistry: Diverse Chemical Function from a Few Good Reactions

scientific article (publication date: June 2001)

Click chemistry in materials synthesis. III. Metal-adhesive polymers from Cu(I)-catalyzed azide-alkyne cycloaddition

Click-Chemie: diverse chemische Funktionalität mit einer Handvoll guter Reaktionen

scientific article from 2001

Copper(I)-catalyzed cycloaddition of organic azides and 1-iodoalkynes

scientific article

Copper(I)-catalyzed synthesis of azoles. DFT study predicts unprecedented reactivity and intermediates

scientific article

Design and synthesis via click chemistry of 8,9-anhydroerythromycin A 6,9-hemiketal analogues with anti-MRSA and -VRE activity

scientific article

Dihydroxylation of Polyenes Using Narasaka's Modification of the Upjohn Procedure

scientific article published in October 1998

Effect of isomers of swainsonine on glycosidase activity and glycoprotein processing

scientific article published on 01 May 1987

Efficiency and Fidelity in a Click-Chemistry Route to Triazole Dendrimers by the Copper(I)-Catalyzed Ligation of Azides and Alkynes

scholarly article by Peng Wu et al published 26 July 2004 in Angewandte Chemie International Edition

Electrophilic and nucleophilic organoselenium reagents. New routes to .alpha.,.beta.-unsaturated carbonyl compounds

scientific article published in 1973

Enzymic cyclization of trans,trans,trans-18,19-dehydrosqualene 2,3-oxide ⬇️

scientific article published on 01 December 1967

Ethenesulfonyl Fluoride (ESF): An On-Water Procedure for the Kilogram-Scale Preparation

scientific article published on 20 October 2016

Expanded therapeutic potential in activity space of next-generation 5-nitroimidazole antimicrobials with broad structural diversity

scientific article published on 07 October 2013

Experimental and Theoretical Kinetic Isotope Effects for Asymmetric Dihydroxylation. Evidence Supporting a Rate-Limiting “(3 + 2)” Cycloaddition

article

First Practical Synthesis of Formamidine Ureas and Derivatives ⬇️

scientific article published on 01 May 2003

Freeze-frame inhibitor captures acetylcholinesterase in a unique conformation

scientific article

Generation of Candidate Ligands for Nicotinic Acetylcholine Receptors via in situ Click Chemistry with a Soluble Acetylcholine Binding Protein Template

scientific article

Identification of a new endogenous metabolite and the characterization of its protein interactions through an immobilization approach ⬇️

scientific article published on January 2009

Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification

scientific article

In Situ Click Chemistry for the Identification of a Potent D-Amino Acid Oxidase Inhibitor

scientific article published on 18 December 2015

In situ click chemistry: a powerful means for lead discovery

scientific article

In situ click chemistry: enzyme inhibitors made to their own specifications

scientific article published in October 2004

In situ click chemistry: enzyme-generated inhibitors of carbonic anhydrase II.

scientific article published in December 2004

In situ selection of lead compounds by click chemistry: target-guided optimization of acetylcholinesterase inhibitors

scientific article published in May 2005

Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries

scientific article published on 22 June 2009

Interaction kinetics of oximes with native, phosphylated and aged human acetylcholinesterase

scientific article published on 20 April 2010

Iterative in Situ Click Chemistry Assembles a Branched Capture Agent and Allosteric Inhibitor for Akt1 ⬇️

scientific article published on October 24, 2011

Iterative in situ click chemistry creates antibody-like protein-capture agents

scientific article published on January 2009

Kinetic resolution of racemic allylic alcohols by enantioselective epoxidation. A route to substances of absolute enantiomeric purity?

scientific article published in 1981

Kinetic resolution of racemic olefins via asymmetric dihydroxylation

scientific article (publication date: August 1993)

Ligand-Accelerated Catalysis

Ligand-Dependent Reversal of Facial Selectivity in the Asymmetric Dihydroxylation

scientific article published in November 1996

Lower valent tungsten halides. New class of reagents for deoxygenation of organic molecules

article

Mechanism of asymmetric epoxidation. 2. Catalyst structure

scientific article published in 1991

Mechanism of interaction of novel uncharged, centrally active reactivators with OP-hAChE conjugates ⬇️

scientific article published on September 4, 2012

Mechanisms of tetrazole formation by addition of azide to nitriles

scientific article published in October 2002

Mechanistic studies on the Cu-catalyzed three-component reactions of sulfonyl azides, 1-alkynes and amines, alcohols, or water: dichotomy via a common pathway

scientific article published on 17 June 2008

Modular click chemistry libraries for functional screens using a diazotizing reagent

scientific article published on 02 October 2019

Molar Scale Synthesis of Enantiopure Stilbene Oxide

scientific article published in September 1996

Molecular basis of interactions of cholinesterases with tight binding inhibitors.

scientific article published on 11 November 2005

Multidimensional SuFEx Click Chemistry: Sequential Sulfur(VI) Fluoride Exchange Connections of Diverse Modules Launched From An SOF4 Hub.

scientific article

Multivalent, bifunctional dendrimers prepared by click chemistry

scientific article published on 4 November 2005

NH-1,2,3-Triazole-based Inhibitors of the VIM-2 Metallo-β-Lactamase: Synthesis and Structure-Activity Studies

scientific article published on July 2010

New Structural Scaffolds for Centrally Acting Oxime Reactivators of Phosphylated Cholinesterases ⬇️

scientific article published on April 4, 2011

New reaction. Stereospecific vicinal oxyamination of olefins by alkyl imido osmium compounds

scholarly article by Karl Barry Sharpless et al published April 1975 in Journal of the American Chemical Society

Nucleophilic substitution by grignard reagents on sulfur mustards

scientific article published in October 2004

Observation of the controlled assembly of preclick components in the in situ click chemistry generation of a chitinase inhibitor

scientific article

Olefin synthesis. Rate enhancement of the elimination of alkyl aryl selenoxides by electron-withdrawing substituents

On the timing of hydrolysis / reoxidation in the osmium-catalyzed asymmetric dihydroxylation of olefins using potassium ferricyanide as the reoxidant

scholarly article by Yasukazu Ogino et al published August 1991 in Tetrahedron Letters

Osmium-catalyzed vicinal oxyamination of olefins by N-chloro-N-argentocarbamates

scientific article (publication date: May 1978)

Oxime-assisted Acetylcholinesterase Catalytic Scavengers of Organophosphates That Resist Aging ⬇️

scientific article published on July 5, 2011

Polytriazoles as copper(I)-stabilizing ligands in catalysis

scientific article

Probing gorge dimensions of cholinesterases by freeze-frame click chemistry

scientific article

REGIOSELECTIVE SYNTHESIS OF EITHER 1H- OR 2H-1,2,3- TRIAZOLES VIA MICHAEL ADDITION TO α,ß-UNSATURATED KETONES.

scientific article

Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization

scientific article

Reengineering Antibiotics to Combat Bacterial Resistance: Click Chemistry [1,2,3]-Triazole Vancomycin Dimers with Potent Activity against MRSA and VRE.

scientific article

Refinement of Structural Leads for Centrally Acting Oxime Reactivators of Phosphylated Cholinesterases ⬇️

scientific article published on February 16, 2012

Role of architecture and molecular weight in the formation of tailor-made ultrathin multilayers using dendritic macromolecules and click chemistry

article

Ruthenium-catalyzed cycloaddition of alkynes and organic azides

scientific article

Searching for new reactivity (Nobel lecture).

scientific article published in June 2002

Selective asymmetric dihydroxylation (AD) of dienes

scientific article (publication date: September 1992)

Selective perhydroxylation of squalene: taming the arithmetic demon

scientific article

Selenium dioxide oxidation of endocyclic olefins. Evidence for a dissociation-recombination pathway

article

Selenium dioxide oxidation of ketones and aldehydes. Evidence for the intermediacy of .beta.-ketoseleninic

article

Some reactions of N-(2-hydroxyalkyl)-p-toluenesulfonamides and N-allyl-p-toluenesulfonamides

article

Stereo and regioselective openings of chiral 2,3-epoxy alcohols. Versatile routes to optically pure natural products and drugs. Unusual kinetic resolutions

Steric and Dynamic Parameters Influencing In Situ Cycloadditions to Form Triazole Inhibitors with Crystalline Acetylcholinesterase

scientific article

Structural insights into conformational flexibility at the peripheral site and within the active center gorge of AChE.

scientific article published on 2 November 2005

SuFEx Chemistry of Thionyl Tetrafluoride (SOF4 ) with Organolithium Nucleophiles: Synthesis of Sulfonimidoyl Fluorides, Sulfoximines, Sulfonimidamides, and Sulfonimidates

scientific article published on 4 January 2018

SuFEx-Based Polysulfonate Formation from Ethenesulfonyl Fluoride-Amine Adducts

scientific article published on 18 May 2017

SuFEx-based synthesis of polysulfates

scientific article published on 5 August 2014

Sulfur(VI) fluoride exchange (SuFEx): another good reaction for click chemistry.

scientific article

Synthesis and Crystal Structure of a ChiralC3-Symmetric Monophosphane

article

Synthesis and electrochemistry of 2-ethenyl and 2-ethanyl derivatives of 5-nitroimidazole and antimicrobial activity against Giardia lamblia

scientific article published on July 2009

Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates

scientific article

The Banert Cascade: A Synthetic Sequence to PolyfunctionalNH-1,2,3-Triazoles

The Catalytic Asymmetric Aminohydroxylation of Unsaturated Phosphonates

scientific article published in October 1999

The allylic azide rearrangement: achieving selectivity

scientific article published in October 2005

The first practical method for asymmetric epoxidation

scientific article (publication date: August 1980)

The growing impact of click chemistry on drug discovery

scientific article

The osmium-catalyzed asymmetric dihydroxylation: a new ligand class and a process improvement

scholarly article by Karl Barry Sharpless et al published May 1992 in Journal of Organic Chemistry

Toward an Understanding of the High Enantioselectivity in the Osmium-Catalyzed Asymmetric Dihydroxylation (AD). 1. Kinetics

scholarly article by Hartmuth C. Kolb et al published February 1994 in Journal of the American Chemical Society

Toward an Understanding of the High Enantioselectivity in the Osmium-Catalyzed Asymmetric Dihydroxylation. 4. Electronic Effects in Amine-Accelerated Osmylations

scholarly article by Derek W. Nelson et al published February 1997 in Journal of the American Chemical Society

Using sulfuramidimidoyl fluorides that undergo sulfur(VI) fluoride exchange for inverse drug discovery

scientific article published on 31 August 2020

Why is tetrazole formation by addition of azide to organic nitriles catalyzed by zinc(II) salts?

scientific article published in August 2003

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