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Method for the synthesis of irinotecan
专利权人:
Synbias Pharma AG
发明人:
Alexander Zabudkin,Viktor Matvienko
申请号:
US15023827
公开号:
US09765083B2
申请日:
2014.11.24
申请国别(地区):
US
年份:
2017
代理人:
摘要:
The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.
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