发明授权
- 专利标题: Processes and intermediates for quinine, quinidine, isomers and derivatives thereof
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申请号: US38455673申请日: 1973-08-01
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公开(公告)号: US3914235A公开(公告)日: 1975-10-21
- 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: US38455673 1973-08-01; US10478471 1971-01-07; US21277471 1971-12-27; US74191468 1968-07-02; US83735469 1969-06-27
- 主分类号: C07D211/32
- IPC分类号: C07D211/32 ; C07D211/34 ; C07D211/76 ; C07D211/94 ; C07D217/06 ; C07D401/12 ; C07D453/04 ; C07D471/04 ; C07D215/12
摘要:
The preparation of quinine, quinidine, isomers and derivatives thereof from the correspondingly substituted 4-methylquinoline and 1-acyl(or 1-H)-3-vinyl(or lower alkyl)-4-piperidine acetic acid esters (or acetaldehyde) through alternative series of reaction steps which comprise, condensation, halogenation, deacylation, reduction, cyclization and hydroxylation, is described. Also described is the preparation of 1-acyl(or 1-H)-3vinyl-4-piperidineacetic acids and esters thereof and 1-acyl-3vinyl-4-piperidineacetaldehyde utilizing the corresponding 7acyldecahydro-2H-pyrido(3,4-d)azepin-2-one, prepared from 2-acyl1,3,4,7,8,8a-hexahydro-6(2H)-isoquinolone. The end products are useful as antimalarial and antiarrhythmic agents.
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