The Scripps Research Institute

Bristol-myers Squibb Compnay

Other

Ika-werke Gmbh & Co. Kg

Eisai R&d Management Co., Ltd.

Phil Baran

Martin D Eastgate

Bin Zheng

Michael Anthony Schmidt

Kyle Knouse

Richard Eric Olson

William R Ewing

Arnab Kumar Chatterjee

Kristen Johnson

Evan J Horn

Manoj Kumar

Dirk Waldmann

Chao Li

Jie Wang

Shan Yu

Justine deGruyter

Tian Qin

Ming Shang

Francis Gerard Fang

Jun Shi

Charles E Chase

Ivar M McDonald

Carlos A Guerrero

Ivar M Mcdonald

Ryan Shenvi

Nazaret Rivas-bascón

Natalia M Padial

Julien C Vantourout

Susana Valente

Janice Akemi Dixon

Ryan Baxter

Yuta Fujiwara

Chuang-Chuang Li

Dongmin Xu

Ryan A Shenvi

The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.

Reagents and their use for modular enantiodivergent synthesis of C—P bonds

The invention is directed to methods of converting a carboxylic acid group in a compound, via a redox active ester, to a corresponding boronic ester by treatment with bis(pinacolato)diboron-alkyllithium complex in the presence of a ligand, a Ni(II) salt or a copper salt, and an Mg(II) salt, in the presence of an alkyllithium or a lithium hydroxide or alkoxide salt. The product pinacolato boronate ester can be cleaved to provide a boronic acid. The invention is also directed to methods of preparing various compounds of medical value comprising boronic acid groups, and to novel boronic-acid containing compounds of medicinal value, including an atorvastatin boronic acid analog, a vancomycin aglycone boronic acid analog, and boronic acid containing elastase inhibitors mCBK319, mCBK320, mCBK323, and RPX-7009.

Cu- and Ni-catalyzed decarboxylative borylation reactions

The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.

Phosphorus (V)-based reagents, processes for the preparation thereof, and their use in making stereo-defined organophosphorus (V) compounds

Phosphorous (V)-based reagents, processes for the preparation thereof, and their use in making stereo-defined organophoshorous (V) compounds

The invention is directed to methods of converting a carboxylic acid group in a compound, via a redox active ester, to a corresponding boronic ester by treatment with bis(pinacolato)diboron-alkyllithium complex in the presence of a ligand, a Ni(ll) salt or a copper salt, and an Mg(ll) salt, in the presence of an alkyllithium or a lithium hydroxide or alkoxide salt. The product pinacolato boronate ester can be cleaved to provide a boronic acid. The invention is also directed to methods of preparing various compounds of medical value comprising boronic acid groups, and to novel boronic-acid containing compounds of medicinal value, including an atorvastatin boronic acid analog, a vancomycin aglycone boronic acid analog, and boronic acid containing elastase inhibitors mCBK319, mCBK320, mCBK323, and RPX-7009.

The invention relates to a closure for an electrochemical reaction vessel, in particular a potentiostat, the closure comprising: a holder for holding electrodes arranged at an inner side of the closure such that, when the closure is attached to a reaction vessel, electrodes held by the holder extend into an interior space of the reaction vessel and into an electrolyte contained in the reaction vessel; and a plurality of contacts arranged at an outer side of the closure for providing electrical contacts with the electrodes.

Closure for an electrochemical vessel, electrochemical vessel and laboratory device

The invention relates to methods and intermediates useful in the synthesis of eribulin.

Intermediates in the synthesis of eribulin and related methods of synthesis

Methods for preventing or treating retroviral infection, such as human immunodeficiency virus, in vivo utilize transcriptional inhibitory compounds. These include cortistatin A and analogs of the cortistatin family.

Inhibitors of retroviral replication

A reagent for carrying out a difluoromethylation reaction of unsaturated compounds and ring-nitrogen-containing aromatic compounds, a zinc difluoro-methanesulfinate, as well as a method for making the reagent and a method for its use are disclosed.

Difluoromethylation of unsaturated compounds

An in vitro synthesis of (+) cortistatin A from readily available precursors is disclosed, as are the syntheses of related 17-aryl substituted compounds, the 17-aryl substituted compounds themselves and novel compounds useful in their preparation.

Synthesis of (+) cortistatin A and related compounds

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San Diego, CA, United States of America

Phil Baran