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1. 发明授权

US07683170B2 Methods for preparing Irinotecan 失效
标题翻译：伊立替康的制备方法
公开(公告)号：US07683170B2
公开(公告)日：2010-03-23
申请号：US11608946
申请日：2006-12-11
申请人： Friedrich Wissmann , Holger Rauter , Silvia Werner
发明人： Friedrich Wissmann , Holger Rauter , Silvia Werner
IPC分类号： C07D489/00
CPC分类号： C07D491/22
摘要： Methods for manufacturing 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxy-camptothecin are described comprising I. reacting a mixture of 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride and 7-ethyl-10-hydroxycamptothecin in a polar aprotic solvent with a base in the presence of catalytic amounts of a N-containing cyclic organic compound having 3 to 20 carbon atoms and optionally in the presence of a water binding agent in an amount which effectively binds any water present in the above reactants and solvents; or II. reacting: (a) 7-Ethyl-10-hydroxycamptothecin in a polar aprotic solvent with phosgene, trichlormethyl-chloroformate, bis(trichloromethyl)carbonate or a alternative to phosgene and a base in the presence of catalytic amounts of a N-containing cyclic organic compound having 3 to 20 carbon atoms; and (b) subsequently with piperidinopiperidine and an amine base.
摘要翻译：描述了制备7-乙基-10- [4-（1-哌啶子基）-1-哌啶子基]羰基氧基喜树碱的方法，其包括：将1-氯羰基-4-哌啶基哌啶盐酸盐和7-乙基-10- 羟基喜树碱在极性非质子溶剂中与碱在催化量的含3-20个碳原子的含N环状有机化合物存在下，任选地在水结合剂存在下，其量有效地结合存在于以上反应物和溶剂; 或II。反应：（a）在极性非质子溶剂中的7-乙基-10-羟基喜树碱在光气，三氯甲基氯甲酸酯，双（三氯甲基）碳酸酯或碳酰氯和碱的替代物存在下，在催化量的含氮环状有机物具有3-20个碳原子的化合物; 和（b）随后与哌啶基哌啶和胺基。

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