Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharmaceuticals, Inc.

Guisheng Li

Chris Hugh Senanayake

Ming Shen

Zhi-Hui Lu

Frank Roschangar

Sonia Rodriguez

Jianxiu Liu

Li Feng Zhang

Nathan K Yee

Nizar Haddad

Xiao-Jun Wang

Zhulin Tan

Nitinchandra D Patel

Bo Qu

Yongda Zhang

Daniel Robert Fandrick

Jean-Nicolas Desrosiers

Joshua Daniel Sieber

Ahmad Khodabocus

Vittorio Farina

Zhi-Hui (Bruce) Lu

This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands.

Chiral dihydrobenzooxaphosphole ligands and synthesis thereof

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

Process for making heteroaryl amine intermediate compounds

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

Process for cross coupling indoles

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

Guisheng Li