Boehringer Ingelheim International Gmbh

Apsinterm LLC

Enanta Pharmaceuticals, Inc.

Zhi-Hui Lu

Chris Hugh Senanayake

Yongda Zhang

Frank Roschangar

Guisheng Li

Ahmad Khodabocus

Ming Shen

Dhileepkumar Krishnamurthy

Zhengxu Han

Wenjie Li

Jianxiu Liu

Hanxun Wei

Yat Sun Or

Zhe Wang

Zhenwei Miao

Ying Sun

Richard John Varsolona

Jinhua Jeff Song

Zeren Wang

Jonathan Timothy Reeves

Suanne Nakajima

Daniel Robert Fandrick

Joe Ju Gao

Shirlynn Chen

Danping Li

Rolf-Stefan Brickl

Chitra Telang

Frank X H Wu

Keith R Fandrick

Diana Reeves

Siddharthya Mujumdar

Mayur Suryakant Dudhedia

Jihchin Chung

Diane Crimhilda Reeves

Disclosed are a process and catalysts useful for carrying out asymmetric methlyallylations. The catalysts used in the invention have the formula (IV): wherein X, X, Rand Rare as defined herein. Compounds made by the process of the invention can be used to prepare pharmaceutically active compounds such as 11-&#x3b2;-hydroxysteroid hydrogenase type 1 (11-&#x3b2;-HSD1) inhibitors including 1,3-disubstituted oxazinan-2-ones. 

Process for asymetric methylallylation in the presence of a 2,2'-substituted 1,1&#x2032;-BI-2-naphthol catalyst

Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and Rto Rare as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-&#x3b2;-hydroxysteroid hydrogenase type 1 (11-&#x3b2;-HSD1) inhibitors.

Methods of making diastereomeric organic compounds

This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: 

Solid state forms of a potent HCV inhibitor

Disclosed are syntheses of 11&#x3b2;-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes). 

Synthesis of inhibitors of 11&#x3b2;-hydroxysteroid dehydrogenase type 1

Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of

Process for preparing 2,3-disubstituted indoles

Disclosed are processes for making 2,3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of

Disclosed are 2-bromoaniline or 2-chloroaniline compounds of formula (I): wherein R, Rand X are as defined. The compounds are useful as intermediates for preparing indole compounds.

2-Bromoanaline and 2-chloroaniline compounds

This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.

Method of preparing amine stereoisomers

The present invention provides a process for making a compound of general formula I: wherein: and as described herein.

Process for cross coupling indoles

This invention provides a method of preparing amine stereoisomers, which comprises stereoselectively reducing a sulfinylimine that bears on the sulfinyl group a residue of an alcohol, thiol or amine, or reacting a sulfinylimine stereoisomer that bears on the sulfinyl group a residue of an alcohol, thiol or amine with a source of a nucleophile, to afford a sulfinylamine stereoisomer, followed by contacting the sulfinylamine stereoisomer with a reagent suitable for the cleavage of a sulfur-nitrogen bond, to afford an amine stereoisomer. It also provides novel intermediates useful in the method, and the use of certain of the intermediates in the preparation of sulfoxide and sulfinylamine stereoisomers.

The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Aza-peptide macrocyclic hepatitis C serine protease inhibitors

The present invention provides a method for making substituted indole compounds of general formula III comprising the step of: (a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I) (I)wherein: X, R and Rare defined hereinwith a substituted acetylene of formula (II) wherein Rand Rare defined herein in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III); 

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Zhi-Hui Lu