Boehringer Ingelheim International Gmbh

Yongda Zhang

Chris Hugh Senanayake

Zhi-Hui Lu

Nathan K Yee

Xiao-Jun Wang

Sonia Rodriguez

Bo Qu

Daniel Robert Fandrick

Jean-Nicolas Desrosiers

Joshua Daniel Sieber

Li Feng Zhang

Nizar Haddad

Zhulin Tan

Nitinchandra D Patel

Wenjie Li

Guisheng Li

Ahmad Khodabocus

Hanxun Wei

Jinhua Jeff Song

Jonathan Timothy Reeves

Joe Ju Gao

Keith R Fandrick

Diana Reeves

Hari P R Mangunuru

Kendricks Lao

Soumik Biswas

Hari PR Mangunuru

Diane Crimhilda Reeves

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

Chiral dihydrobenzoazaphosphole ligands and synthesis thereof

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

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

Growing community of inventors

Sandy Hook, CT, United States of America

Yongda Zhang