Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharmaceuticals, Inc.

Boehringer Ingelheim Pharma Gmbh & Co Kg

Jianxiu Liu

Chris Hugh Senanayake

Guisheng Li

Ming Shen

Nathan K Yee

Xudong Wei

Suresh R Kapadia

Nizar Haddad

Carl Alan Busacca

Fabrice Gallou

Zhi-Hui Lu

Frank Roschangar

Azad Hossain

Sonia Rodriguez

Vittorio Farina

Zhi-Hui (Bruce) Lu

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 are processes to produce a compound of the formula (I): 

Process for making heteroaryl amine intermediate compounds

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 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

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); 

Palladium catalyzed indolization of 2-bromo or chloroanilines

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Richmond, VA, United States of America

Jianxiu Liu