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N- [ (2 ` R) -2 ` -DEOXY-2 ` -FLUORO-2 ` -METHYL-P-PHENYL-5 ` -URIDYLYL] -L-ALANINE 1-METHYLETHYL ESTER AND PROCESS FOR ITS PRODUCTION
专利权人:
PHARMASSET; INC
发明人:
ROSS, BRUCE, S,SOFIA, MICHAEL, JOSEPH,PAMULAPATI, GANAPATI, REDDY,RACHAKONDA, SUGUNA,ZHANG, HAI-REN,CHUN, BYOUNG-KWON,WANG, PEIYUAN
申请号:
PH12015502237
公开号:
PH12015502237A1
申请日:
2015.09.24
申请国别(地区):
PH
年份:
2016
代理人:
摘要:
Disclosed herein are nucleoside phosphoramidates of formula 4 and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals. Disclosed is also a process for preparing compound represented by formula 4: (Formula 4) wherein P* represents a chiral phosphorus atom, which comprises: a) reacting an isopropyl-alanate, (Formula A), a di-X'-phenylphosphate, (Formula B), 2'-deoxy-2f-fluoro-2'-C-methyluridine, (Formula 3), and a base to obtain a first mixture comprising 4; wherein X is a conjugate base of an acid, n is 0 or 1, and X' is a halogen, b) reacting the first mixture with a protecting compound to obtain a second mixture comprising 4; and c) optionally subjecting the second mixture to crystallization, chromatography or extraction in order to obtain 4.
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中国工程科技知识中心
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http://www.ckcest.cn/home/

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