Schering Corporation

Merck Sharp + Dohme Corp.

Schering-plough Corporation

Eugene John Vater

Jeonghan Park

Anantha R Sudhakar

Minzhang Chen

Richard W Draper

Xiaojing Yang

Weidong Tong

Ramani R Raghavan

Juergen Weber

Ingyu Jeon

Maria M Tamarez

George S K Wong

Daw-long Albert Kwok

George S Wong

Yuelie Lu

Daw-Jong Kwok

Shuan Dong

Radha V Iyer

A process for preparing 3-amino-3-cyclobutylmethyl-2-hydroxypropionamide of the Formula I: or a salt thereof involves providing a compound of the Formula VI described herein in a solution comprising predominately dimethylsulfoxide (DMSO) and converting this compound directly to the compound of the Formula VIII described herein without working up or isolating the intermediate compound of the Formula VII described herein.

Process for the synthesis of 3-amino-3-cyclobuthylmethyl-2-hydroxypropionamide or salts thereof

In one embodiment, the present application relates to a process of making a compound of formula I. and to certain intermediate compounds that are made within the process of making the compound of formula I.

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Process and intermediates for the preparation of (1R,2S,5S)-6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylates for salts thereof

Process and intermediates for the preparation of (1R,2S,5S)-6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylates or salts thereof

A short practical commercial process for the efficient enantioselective synthesis of the non-steroidal antiestrogen of formula I or XIV

Enantioselective synthesis

Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethylformamide; at a temperature within the range of about -78.degree. to about 0.degree. C.

Process for preparation of 9.alpha. -chloro-11.beta.

Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethyl formamide; at a temperature within the range of about -78.degree. to about 0.degree. C., under anhydrous conditions under an inert atmosphere.

Process for preparation of

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Lyndhurst, NJ, United States of America

Eugene John Vater