Genentech, Inc.

Other

Sumitomo Chemical Company, Limited

F. Hoffmann-la Roche Ag

Zhigang Cheng

Srinivasan Babu

Qingping Tian

Mark E Reynolds

Herbert Yajima

Francis Gosselin

Scott J Savage

Reinhard Reents

Ursula Hoffmann

Pirmin Hidber

Andrew McClory

Takashi Miki

Theresa Humphries

Yasuharu Shimasaki

Andrew Mcclory

A process for the manufacture N-(5-((5R,6S)-5-amino-6-fluorooxepan-2-yl)-1-methyl-1H-pyrazol-4-yl)-2-(2,6-difluorophenyl)thiazole-4-carboxamide (I) wherein the vicinal amino fluoro substituents are introduced by treating 5 with sodium chloro((4-nitrophenyl)sulfonyl)amide and N-bromosucinimide and unraveling the resulting substituted aziridine (6) with trimethylamine trihydrofluoride to afford 7 which is further processed to afford 1. 

Process for the preparation of a medicament

Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure:  and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.

Process for making thienopyrimidine compounds

The present invention relates to a method for manufacturing a boronic acid ester compound, characterized by reacting an aryl halide compound and a diboron ester compound in the presence of a nitrogen-containing organic base, a nickel catalyst, a phosphine compound and a solvent. According to the manufacturing method of the present invention, even if a nickel catalyst is used as the catalyst, a desired boronic acid ester compound can be obtained in a sufficiently high yield. Furthermore, even if aryl chloride or aryl bromide having relatively low price and low reactivity, was used as the aryl halide compound, a desired boronic acid ester compound can be obtained in a sufficiently high yield.

Method for manufacturing a boronic acid ester compound

The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.  

The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula (I) and (II) compounds, and novel intermediates for preparing Formula (I) and (II) compounds. 

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South San Francisco, CA, United States of America

Zhigang Cheng