发明授权
- 专利标题: Intermediates for quinine, quinidine and derivatives thereof
- 专利标题(中): 奎宁,奎尼丁及其衍生物的中间体
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申请号: US35483873申请日: 1973-04-26
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公开(公告)号: US3869461A公开(公告)日: 1975-03-04
- 发明人: GUTZWILLER JUERG ALBERT WALTER , USKOKOVIC MILAN RADOJE
- 申请人: HOFFMANN LA ROCHE
- 专利权人: Hoffmann La Roche
- 当前专利权人: Hoffmann La Roche
- 优先权: US35483873 1973-04-26; US10478571 1971-01-07; US21264871 1971-12-27; US74191368 1968-07-02; US83730469 1969-06-27
- 主分类号: C07D401/06
- IPC分类号: C07D401/06 ; C07D33/50
摘要:
Quinine, quinidine, their antipodes or racemates and derivatives thereof, are prepared by (a) cyclizing the correspondingly substituted 4-(3-(1-chloro-3(R)-alkyl(or alkenyl)-4(R)piperidyl)-1-oxopropyl)quinolines, antipodes or racemates thereof, to the corresponding 4-(5(R)-alkyl(or alkenyl)-4(S)quinuclidin-2(S) or 2(R)-ylcarbonyl)quinolines, antipodes or racemates thereof; and (b) stereoselectively reducing the products of step (a) to Alpha (S)-(5(R)-alkyl(or alkenyl)-4(S)quinuclidin-2(R)-yl)-4-quinolinemethanols, antipodes or racemates thereof, and Alpha (R)-(5(R)-alkyl(or alkenyl)-4(S)-quinuclidin2(S)-yl)-4-quinolinemethanols, antipodes or racemates thereof. Various intermediates and the end products are useful antimalarial and antiarrhythmic agents.
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