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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:
Gilead Pharmasset LLC
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:
AU2016200676
公开号:
AU2016200676A1
申请日:
2016.02.03
申请国别(地区):
AU
年份:
2016
代理人:
摘要:
#$%^&*AU2016200676A120160225.pdf#####1000855157 Abstract 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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