Patent ID: 7728135
Filing Date: 2010-06-01
Classification: A61P,C07D

Abstract:
1. A process for preparing a compound of formula (I) from a compound of formula V: where X and Y are suitable protective moieties, wherein said process comprises: (a) selectively removing the X protecting group of the compound of formula V to produce a compound of formula VI: (b) sulfonylating the compound of formula VI with a cyclopropyl sulfonyl moiety, where W is a first leaving group:  to form the compound of formula VII: (c) removing the Y protecting group from the compound of formula VII and reacting with hydrogen bromide to produce the di-hydrobromide salt formula VIII: (d) reacting the compound of formula VIII with (i) an agent containing a leaving group G where G is a second leaving group selected from the group consisting of CN, Z, alkylsulfonates, OCOCZ to form the compound of formula IX: and (e) reacting the compound of formula IX with a Grignard reagent in a suitable solvent, followed by workup, to yield the compound of formula I, with the proviso that X and Y are different such that X may be selectively removed.