Boehringer Ingelheim International Gmbh

Novartis Ag

Other

Boehringer Ingelheim Pharmaceuticals, Inc.

Boehringer Ingelheim Pharma Gmbh & Co Kg

Anadys Pharmaceuticals, Inc.

Fabrice Gallou

Nathan K Yee

Chris Hugh Senanayake

Xudong Wei

Nizar Haddad

Jianguang Zhou

Carl Alan Busacca

Jinghua Xu

Pengfei Guo

Michael Parmentier

Jinhua Jeff Song

Suresh R Kapadia

Zhulin Tan

Li Feng Zhang

Philipp Lustenberger

Bo Han

Jianxiu Liu

Yibo Xu

Feng Gao

Said Saim

Rogelio Perez Frutos

Xiao-Jun Wang

Thomas Nicola

Robert Simpson

Juergen Schnaubelt

Bernard Riss

Hans Stettler

Azad Hossain

Joerg Brandenburg

Dirk Kemmer

Christian Mathes

Yu Gai

Dieter Gutheil

Weiyong Kong

Jutta Kroeber

Vittorio Farina

Kai Oliver Donsbach

Caspar Vogel

Heewon Lee

Michael Schul

Robert Hagenkoetter

Franck Mallet

Hans-Dieter Ecker

Joerg Matthias Sedelmeier

Eric Winter

Qiangbiao Pan

Hao Wang

Benli Zou

Jiong Ye

Matthias Napp

Dietmar Flubacher

Michael Haller

Pascal Beney

The present invention is directed to reaction mixtures comprising a water-surfactant mixture, wherein the catalyst comprises a compound with solubilizing groups. This technology improves the solubility of the reaction components in the water-surfactant mixture and thereby, greatly increases the productivity and selectivity of the chemical reaction.

Catalysts for chemical reactions in a water-surfactant mixture

The present invention is directed to reaction mixtures comprising a water-surfactant mixture and a co-solvent. This technology reduced the amount of organic solvents needed for performing chemical reactions. Furthermore, compared to reaction mixtures lacking the co-solvent, solvation of the reactants and products of the chemical reaction is greatly enhanced, leading to a significantly improved yield, purity, reproducibility and robustness.

Reaction medium containing water-surfactant mixture

The present invention is directed to aqueous reaction mixtures for enzymatic synthesis reactions comprising a surfactant. The surfactant in the reaction mixture increases stability and yield of the enzymatic reaction. Furthermore, method for performing an enzymatic reaction using said aqueous reaction mixtures are provided.

Enzymatic reaction medium containing surfactant

This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.

Process for preparing 1-(4-methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo [2,3-B]pyridin-3-yl-acetic acid

The present invention relates to processes and intermediates useful for the manufacture of cyclic undecapeptides, such as Alisporivir.

Process for the manufacture of cyclic undecapeptides

This invention relates to novel processes for synthesizing N-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester and to the compound of formula I below and other intermediates that are used in such processes. 

Process for preparing N-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester

Disclosed is a process for preparing a macrocyclic compound of the formula (I) wherein a hydroxyl-substituted macrocyclic compound of formula (3) is reacted with a sulfonyl-substituted compound of formula QUIN:  The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

Process for preparing macrocyclic compounds

Disclosed is a process for preparing substituted anisidines of formula I starting from substituted cyclic hydroxy-ketones II via aromatization through a substituted oxime intermediate IV in which R is C-Calkyl or halogen, and Alk is C-Calkyl. The substituted anisidines of formula I have been found to be useful as intermediates in the preparation of agents for the treatment of hepatitis C viral (HCV) infections. 

Process for preparing substituted anisidines

Intermediates of the formula QUIN: and methods for their preparation are described. The intermediate compounds are useful for preparing active agents for the treatment of hepatitis C virus (HCV) infection.

Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I): wherein Q is a radical of the following formula: and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: 

Process for preparing macrocyclic HCV protease inhibitors

A process for removing ruthenium or ruthenium-containing compounds from a reaction mixture comprising a compound of the following formula I in an organic solvent using supercritical fluid processing techniques: wherein R, R, R, D and A are as defined herein. This invention has particular application for removing ruthenium-containing catalyst and ruthenium-containing catalyst by products from reaction mixtures that result from ring-closing olefin metathesis (RCM) reactions.

Removal of ruthenium by-product by supercritical fluid processing

Disclosed is a process for preparing a compound of formula I comprising cyclizing a diene compound of formula III in the presence of a ruthenium catalyst in a suitable organic solvent, wherein the process is performed in a gaseous fluid at supercritical or near-supercritical conditions: The compounds of formula (I) are active agents for the treatment of hepatitis C viral (HCV) infections or are intermediates useful for the preparation of anti-HCV agents.

Ring-closing metathesis process in supercritical fluid

A process for stereoselective synthesis of a compound of Formula (I) wherein R, R, R, R, and Rare as described herein.

Stereoselective synthesis of certain trifluoromethyl-substituted alcohols

Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, Rthrough R, D, A and Rare as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

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Basel, Switzerland

Fabrice Gallou