N-[(2&rsquo；r)-2&rsquo；-deoxy-2&rsquo；-fluoro-2&rsquo；-methyl-p-phenyl-5&rsquo；-uridylyl]-l-alanine 1-methylethyl ester and process for its production

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专利权人:

GILEAD PHARMASSET LLC

发明人:

WANG PEIYUAN,SOFIA MICHAEL JOSEPH,PAMULAPATI GANAPATI REDDY,ZHANG HAI-REN,CHUN BYOUNG-KWON,ROSS BRUCE S.,RACHAKONDA SUGUNA

申请号：

NZ62360210

公开号：

NZ623602A

申请日:

2010.05.20

申请国别(地区):

NZ

年份:

2015

代理人:

摘要：

Disclosed is the enantiomeric purification of (S)-2-[(S)-(4-nitro-phenoxy)-phenoxy-phosphorylamino]propionic acid isopropyl ester and its analogues as useful synthetic intermediates in the enantiomerically pure synthesis of sofosbuvir. Also disclosed are compounds of general formula C and C&rsquo；, wherein R is a leaving group (LG&rsquo；) selected from tosylate, camphorsulfonate, an aryloxide, or an aryloxide substituted with at least one electron withdrawing group, and preferably selected from p-nitrophenoxide, p-chlorophenoxide, o-chlorophenoxide, 2,4-dinitrophenoxide and pentafluorophenoxide.

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