发明名称 |
Process for producing derivatives of 4a,5,9,10,11,12,-hexahydro- 6H-benzofuro[3a,3,2-ef][2]benzazepine |
摘要 |
<p>The proposal is for a process for producing derivatives of 4a,5,9,10,11,12,-hexahydro-6H-benzofuro[3,2-ef][2]benzazepine facilitating in particular the production of galanthamine (6) via the novel bromine-N-demethyl galanthamine (4) and the novel bromine galanthamine (5). In this process, the compound (2) is oxidatively cyclised into the compound (3). The compound (3) is diastereo-selectively reduced by L-selectrides to the novel bromine-N-demethyl galanthamine (4) without the formation of detectable quantities of epibromine-N-demethyl galanthamine. The novel bromine galanthamine (5) is obtained by methylation, from which by separation of bromine (+/-) galanthamine (6) is produced. Pure enantiomers can be demonstrated by precipitation as a salt of a chiral acid (especially a tartrate). The process shown in the reaction diagram below gives high yields and pure products at all stages and can thus be conducted on the industrial scale.</p> |
申请公布号 |
SK283877(B6) |
申请公布日期 |
2004.04.06 |
申请号 |
SK19970000483 |
申请日期 |
1995.10.23 |
申请人 |
SANOCHEMIA PHARMAZEUTIKA AG |
发明人 |
CZOLLNER LASZLO;FROHLICH JOHANNES;JORDIS ULRICH;KUENBURG BERNHARD |
分类号 |
C07D491/048;C07B53/00;C07B57/00;C07C217/58;C07D223/00;C07D307/00;C07D491/00;C07D491/06;C07D491/10;C07D491/153;C07D491/20;(IPC1-7):C07B53/00 |
主分类号 |
C07D491/048 |
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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