Bristol-myers Squibb Compnay

Albany Molecular Research, Inc.

Britsol-myers Squibb Company

Paul C Lobben

Benjamin Cohen

Shuang Liu

Bang-Chi Chen

Rulin Zhao

Martin D Eastgate

Chiajen Lai

Yi Xiao

Qi Gao

Gregory L Beutner

Michael Shawn Lawler

David Kenneth Leahy

Bin Zheng

Lori Ann Spangler

Matthew L Isherwood

Nicolas Cuniere

Christopher S Regens

Jaan A Pesti

Wenge Cui

Francis S Gibson

Min Hu

Gerard Crispino

Bei Wang

Thorsten Rosner

Lopa V Desai

Carolyn S Wei

John E Thornton

Gerard A Crispino

Neil A Strotman

Rasidul Amin

Keming Zhu

Zhongmin Xu

Yuh-lin Allen Yang

Robert P Discordia

Mourad Hamedi

Jale Muslehiddinoglu

Thomas L LaPorte

Michael Bryan Hay

Monica Fitzgerald

Thomas L Laporte

David K Leahy

The invention relates to an improved process for synthesizing N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide of the formula: (I) Compound (I) is currently in clinical trials for the treatment of myeloproliferative disorders, such as polycythaemia vera, thrombocythaemia and primary myelofibrosis. 

Process for the preparation of N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide

Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form. One such intermediate has the following structure: 

Tetrahydroisoquinolines and intermediates therefor

The invention relates to an improved process for preparing [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula:  Compound I has been shown to be useful for the treatment of certain types of cancer.

Process for the preparation of [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2, 1-F][1,2,4]triazin-6-yloxy]-1-methylethyl ester

A method for preparing a compound having the formula:  to form a compound of formula I: 

Methods for the preparation of pyrrolotriazine compounds

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Lawrenceville, NJ, United States of America

Paul C Lobben