SUGUNA RACHAKONDA,GANAPATI REDDY PAMULAPATI,BRUCE S. ROSS,MICHAEL JOSEPH SOFIA,HAI-REN ZHANG
申请号：
MX2012011324
公开号：
MX2012011324A
申请日:
2011.03.31
申请国别(地区):
MX
年份:
2013
代理人:
摘要：
Disclosed herein are phosphorus-containing actives, their use as actives for treating diseases, and a stereoselective process for preparing the same. Also disclosed herein are useful synthetic intermediates and processes for preparing the same. A process for preparing a composition comprising an enantiomerically- or a diastereomerically-enriched phosphorus-containing active, salt, or pharmaceutically acceptable salt thereof, of formula I is disclosed: 1 which comprises a) reacting a protected or unprotected Active with a base to form a salt of said active and then reacting said salt with an enantiomerically- or a diastereomerically enriched compound of formula II wherein Group is as defined herein, W is an aryl or -CCH<；sub>；2<；/sub>；)nSC(O)C(CH<；sub>；3<；/sub>；)m(CH<；sub>；2<；/sub>；OH)<；sub >；3-m<；/sub>；, where n is 2 or 3 and m is 0, 1, 2, or 3, and LG is a leaving group； b) optionally deprotecting the compound obtained in step a) and c) optionally subjecting the compound obtained in step a) or the compound obtained in step b) to chromatography, extraction, or crystallization to obtain the active.Se describen activos que contiene fósforo, su uso como activos para tratar enfermedades, y un proceso estereoselectivo para preparar los mismos. También se describen intermediarios sintéticos útiles y procesos para prepararlos.
