Pfizer Corporation

Harry A Watson, Jr

Constantine Sklavounos

Douglas J Allen

Robert W McLaughlin

Jonathan B Zung

Brian Thomas O'Neill

Donald E Kuhla

Tamim F Braish

Michael P Deninno

Michael J Castaldi

Stephen S Massett

Glenn E Wilcox

William M Snyder

Richard A Buzon

A method for removing impurities from racemic cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol and purified cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol useful as an estrogen agonist/antagonist.

Purified racemic lasofoxifene and purified lasofoxifene D-tartrate and a method for effective purification of racemic lasofoxifene

The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active substituted 2-phenyl-3-benzylaminopiperidines. The substituted 2-phenyl-3-benzylaminopiperidines that can be prepared by the processes of this invention are substance P receptor antagonists and are useful in the treatment and prevention of inflammatory and central nervous system disorders, as well as several other disorders.

Pharmaceutical agents for the treatment of emesis

Process for preparing derivatives of azabicyclo naphthyridine carboxylic

Crystalline spirostanyl glycosides and processes for making them are disclosed. The crystalline spirostanyl glycosides are useful for treatment of hypercholesterolemia or atherosclerosis.

Spirostanyl glycosidal crystals

Spirostanyl glycosidal crystalline monohydrate

The present process produces the meso dialkyl 2,5-dihaloadipate from a mixture of the racemic dialkyl 2,5-dihaloadipate and meso 2,5-dihaloadipate. In the disclosed process, a 2,5-dihaloadipoyl halide is formed under conditions which result in the formation of an acidic compound. The 2,5-dihaloadipoyl halide is then esterified under conditions wherein the ester of the dihaloadipoyl halide is allowed to remain in contact with the acidic compound, thus allowing the racemic diester to epimerize in the presence of the acidic compound to the meso form and then the meso diester spontaneously crystallizes. In the last stage, the meso diester produced is removed.

Process for the preparation of meso 2,5-dihaloadipates

8-Fluoro-5-(p-fluorophenyl)-2-[4-(p-fluorophenyl)-4-hydroxybutyryl]-2,3,4,5 -tetrahydro-1H-pyrido[4,3-b]-indole; processes therefor; and process for the conversion to flutroline.

Compound,

Trans-N,N-dimethyl-9-[3-(4-methyl-1-piperazinyl)propylidene]-thioxanthene-2 -sulfonamide is isomerized to the cis-isomer by contacting the trans-isomer with strong base in a polar organic solvent. By using an organic solvent in which the solubility of the cis-isomer is substantially less than that of the trans-isomer, the cis-isomer can be selectively precipitated from said solvent, thereby favoring additional isomerization to the cis-isomer in the supernatant, and separated.

Growing community of inventors

Groton, CT, United States of America

Harry A Watson, Jr