Patent ID: 8236959
Filing Date: 2012-08-07
Classification: A61P,C07D

Abstract:
1. A process for preparing the (R,R)—, (S,S)—, (R,S)— or (S,R)-diastereomer of a compound of formula (III) comprising condensing the R or S enantiomer of an oxiranyl compound of formula (I) with the R or S enantiomer of an amine of formula (II) or a salt thereof wherein: R 1 is a group selected from alkyl, aryl, allyl, alkoxy, cycloalkyl, heterocyclic, alkenyl, benzocycloalkyl, aralkyl, haloarylalkyl, heteroaralkyl, haloalkyl, alkoxyaralkyl, and optionally substituted silyl and benzyl; and either (a) R 2 and R 2 ′ are trialkylsilyl and R 3 is hydrogen; (b) R 2 and R 3 are trialkylsilyl and R 2 ′ is hydrogen; (c) R 2 and R 2 ′ are diarylalkylsilyl and R 3 is hydrogen; or (d) R 2 and R 3 are diarylalkylsilyl and R 2 ′ is hydrogen.