Wyeth

Zealand Pharma A/s

Wyeth Holdings Corporation

Karen Sutherland

Panolil C Raveendranath

Jianxin Ren

Lalitha Krishnan

Michael William Winkley

Mahmoud Mirmehrabi

Subodh S Deshmukh

John Leo Considine

Maotang X Zhou

Asaf Ragim Alimardanov

Charles Chao Wu

Jason Brazzillo

Ting-Zhong Wang

Syed Muzafar Shah

Diane H Boschelli

Beat Theodor Weber

Gregg Brian Feigelson

Anthony Francis Hadfield

David Michael Blum

Yanzhong Wu

Mousumi Ghosh

Aeri Park

Mahmut Levent

Henry Strong

James Andrew Provost

Brenton William Russell

Rex A Shipplett

Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.

Synthesis of pyrrolidine compounds

A process for making a compound of formula I and intermediate compounds thereof, wherein Ris CN, F or Cl; Ris H or Br; and Rand Rare each independently H or F. The compounds of formula I are useful in the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.

Process for the synthesis of 3-(3-fluoro-4-hydroxyphenyl)-7-hydroxynaphthonitrile

This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

Process for preparation of 4-amino-3-quinolinecarbonitriles

A novel salt of O-desmethyl venlafaxine is provided, O-desmethylvenlafaxine succinate. Pharmaceutical compositions, dosage forms and methods of use are also provided.

Succinate salt of O-desmethyl-venlafaxine

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New City, NY, United States of America

Karen Sutherland