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A method for the production of piperazine acid and their conversion to n - acylated n, n - linking of the bicyclic rings containing as intermediates for caspase inhibitors

机译：一种制备哌嗪酸并将其转化为含半胱天冬酶抑制剂中间体的双环的n-酰化n，n-连接的方法

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摘要

The invention relates to a process for synthesizing piperazic acid and similar, ring-containing acids. The invention also relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of either or both processes in a method of synthesizing a bicyclic compound useful as an intermediate for the production of an inhibitor of a caspase, particularly an inhibitor of interleukin- β converting enzyme ('ICE').

机译：本发明涉及一种合成哌嗪酸和类似的含环酸的方法。本发明还涉及同时使N（2）酰化哌嗪酸或其酯并形成双环结构的方法。本发明还涉及一种或两种方法在合成双环化合物的方法中的用途，所述双环化合物用作生产胱天蛋白酶的抑制剂，特别是白介素-β转化酶（'ICE'）的抑制剂的中间体。

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公开/公告号DE69917648T2

专利类型
公开/公告日2005-06-09

原文格式PDF
申请/专利权人 VERTEX PHARMACEUTICALS INC. CAMBRIDGE MASS. US;
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申请/专利号DE1999617648T
发明设计人 DIETERICH PETRA WALLINGFORD OXFORDSHIRE OX10 7JN GB;ROBIDOUX L. ANDREA ANDOVER US;STORER NEIL DIDCOT OXFORDSHIRE OX11 7RP GB;LEONARDI STEFANIA WALLINGFORD OXFORDSHIRE OX10 8HW GB;WILSON DOUGLAS JEFFREY BOXFORD US;
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申请日1999-08-19
分类号C07D237/04;C07D487/04;
国家 DE
入库时间 2022-08-21 21:58:51

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