经Ugi四组分缩合反应合成CPP32抑制剂模板

经Ugi四组分缩合反应合成CPP32抑制剂模板

张欣, 邹晓民, 傅翌秋, 杨晓鸣, 牟科, 徐萍^*

北京大学药学院药物化学系, 北京 100083

收稿日期:2004-09-10 修回日期:2004-11-10 出版日期:2004-12-15 发布日期:2004-12-15
通讯作者: 徐萍*

Template Synthesis of CPP32 Inhibitors by Ugi Four-Component Condensation Reaction

ZHANG Xin, ZOU Xiao-min, FU Yi-qiu, YANG Xiao-ming, MOU Ke, XU Ping^*

Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University, Bejing 100083, China

Received:2004-09-10 Revised:2004-11-10 Online:2004-12-15 Published:2004-12-15
Contact: XU Ping*

摘要/Abstract

摘要： 目的　找到合适途径来制备所设计的CPP32抑制剂。方法　Ugi四组分缩合反应用于合成拟肽类CPP32抑制剂。结果　合成了关键异腈组分(天冬氨酸衍生异腈3)和CPP32抑制剂模板分子4。结论　以基于天冬氨酸衍生异腈3的Ugi四组分缩合反应,合成了CPP32抑制剂4。此新建的方法可用于构建CPP32拟肽类抑制剂化学库。

关键词: CPP32, CPP32, CPP32, Ugi4CR, Ugi4CR, Ugi4CR, 异腈, 异腈, 异腈

Abstract: Aim To find a reasonable way to prepare the designed CPP32 inhibitors. Method Ugi four-component condensation reaction was used to synthesize peptide mimic CPP32 inhibitors; Results A key isocyanide component (aspartate-derived isocyanide 3) and one of the designed CPP32 inhibitors 4 (as a template) were synthesized; Conclusion The CPP32 inhibitor 4 was synthesized by the newly developed procedure, which is an Ugi four-component condensation reaction based on aspartate-derived isocyanide 3. This method can be used to build up the CPP32 inhibitor library.

Key words: CPP32, CPP32, Ugi-4CR, Ugi-4CR, isocyanide, isocyanide

中图分类号:

R914.4

Supporting: Foundation item: National Natural Science Foundation of China (20272004) .
^*Corresponding author. Tel.: 86-10-82801505; fax: 86-10-62015584

张欣, 邹晓民, 傅翌秋, 杨晓鸣, 牟科, 徐萍^*. 经Ugi四组分缩合反应合成CPP32抑制剂模板[J]. .

ZHANG Xin, ZOU Xiao-min, FU Yi-qiu, YANG Xiao-ming, MOU Ke, XU Ping^*. Template Synthesis of CPP32 Inhibitors by Ugi Four-Component Condensation Reaction[J]. .

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