ROSS, BRUCE S.,SOFIA, MICHAEL JOSEPH,PAMULAPATI, GANAPATI REDDY,RACHAKONDA, SUGUNA,ZHANG, HAI-REN
申请号：
CA2794671
公开号：
CA2794671C
申请日:
2011.03.31
申请国别(地区):
CA
年份:
2018
代理人:
摘要：
Disclosed herein are phosphorus-containing actives, their use as actives fortreating diseases, and a stereoselectiveprocess for preparing the same. Also disclosed herein are useful syntheticintermediates and processes for preparing the same. Aprocess for preparing a composition comprising an enantiomerically- or adiastereomerically-enriched phosphorus-containing active,salt, or pharmaceutically acceptable salt thereof, of formula I is disclosed:1 which comprises a) reacting a protected or unprotectedActive with a base to form a salt of said active and then reacting said saltwith an enantiomerically- or a diastereomerically enrichedcompound of formula II wherein Group is as defined herein, W is an aryl or -CCH2)nSC(O)C(CH3)m(CH2OH)3-m, where n is 2 or 3and m is 0, 1, 2, or 3, and LG is a leaving group； b) optionally deprotectingthe compound obtained in step a) and c) optionallysubjecting the compound obtained in step a) or the compound obtained in stepb) to chromatography, extraction, or crystallization toobtain the active.
