发明名称 |
Process for preparing piperazinepentaneamide HIV protease inhibitors |
摘要 |
A process for preparing gamma-hydroxy-4-[[2-oxazolyl]alkyl]-alpha-[(cyclo)alkyl- or aryl- or heteroaryl-substituted methyl]-2-[[(un)substituted alkyl]aminocarbonyl]-1-piperazinepentanamides is disclosed. The piperazinepentanamides are useful as HIV protease inhibitors. A process for making a 4-[[2-oxazolyl]alkyl]-2-[[(un)substituted alkyl]aminocarbonyl]piperazine by treating a ketoamide precursor with fuming sulfuric acid in the presence of polyphosphoric acid is also disclosed. In addition, a process for enhancing the optical purity of 4-[[2-oxazolyl]alkyl]-2-[[(un)substituted alkyl]aminocarbonyl]-piperazines via the formation 2-naphthalenesulfonic acid crystal salts thereof is disclosed, as well as a method for purifying 2-naphthalenesulfonic acid.
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申请公布号 |
US2003144512(A1) |
申请公布日期 |
2003.07.31 |
申请号 |
US20020158527 |
申请日期 |
2002.05.30 |
申请人 |
IKEMOTO NORIHIRO;LIU JINCHU |
发明人 |
IKEMOTO NORIHIRO;LIU JINCHU |
分类号 |
C07D413/14;C07D498/04;(IPC1-7):C07D413/14 |
主分类号 |
C07D413/14 |
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