发明名称 |
Process of synthesis of vinblastine and vincristine |
摘要 |
The present invention relates to the synthesis of dimer alkaloid compounds, particularly those of the Catharantus (Vinca) family, from an indole unit, such as cantharanthine, and a dihydroindole unit, such as vindoline. A multi-step process is disclosed including the steps of (1) of 1,4-reduction of a first dimeric iminium intermediate to an enamine compound by reaction with a 1,4-dihydropyridine compound; (2) oxidative transformation of the resulting enamine to a second iminium intermediate under controlled aeration; (3) reduction of the second iminium intermediate to form the target dimer alkaloid compounds. The entire process can be conducted in a one-pot operation to obtain the target compounds without isolation of the intermediates.
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申请公布号 |
US5047528(A) |
申请公布日期 |
1991.09.10 |
申请号 |
US19880228821 |
申请日期 |
1988.08.02 |
申请人 |
UNIVERSITY OF BRISTISH COLUMBIA |
发明人 |
KUTNEY, JAMES P.;CHOI, LEWIS S. L.;NAKANO, JUN;TSUKAMOTO, HIROKI;BOULET, CAMILLE A.;MCHUGH, MICHAEL |
分类号 |
C07D519/04 |
主分类号 |
C07D519/04 |
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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