发明名称 |
Process for preparing optically active piperazine derivatives and intermediates for preparation |
摘要 |
<p>Process for preparing optically active 2-piperazinecarboxylic acid derivatives, particularly S-enantiomer thereof, in high yield and high optical purity on industrial scale. As the optical resolving agents, easily accessible sulfonamides derived from selected optically active amino acids, such as N-tosyl-L-phenylalanine, N-tosyl-D-phenylglycine, N-tosyl-L-alanine or N-tosyl-L-valine, give excellent results. These resolving agents are stable and easily recovered from the reaction mixture and reused. Resolved 2-piperazinecarboxylic acid derivatives are preferably isolated as 4-t-butoxycarbonyl (Boc) derivatives. Diastereomeric salts (an example being shown below) formed as the intermediates of resolution are novel. <CHEM> ÄIn the formula "Ar" stands for a phenyl or naphthyl group which may be substituted with one to three C1-C6 alkyl groups, halogen atoms, nitro or alkoxy groups; and n=0 or 1.Ü</p> |
申请公布号 |
EP0710652(A2) |
申请公布日期 |
1996.05.08 |
申请号 |
EP19950117261 |
申请日期 |
1995.11.02 |
申请人 |
YAMAKAWA CHEMICAL INDUSTRY CO., LTD. |
发明人 |
MURAKAMI, HISAMICHI;SATOH, SHOKO;TOBIYAMA, TADASHI;SAKAI, KEN'ICHI;NOHIRA, HIROYUKI |
分类号 |
C07C311/19;C07D241/04;(IPC1-7):C07D241/04 |
主分类号 |
C07C311/19 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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