经Ugi四组份缩合反应进行α-氨酰基酰胺类化学库的平行合成

经Ugi四组份缩合反应进行α-氨酰基酰胺类化学库的平行合成

徐萍^*, 林文卫, 张婷, 胡兴娥, 邹晓民

1.北京大学药学院药物化学系, 北京 100083;
2.湖北省宜昌卫生学校药学教研室, 宜昌 443000

收稿日期:2000-11-28 修回日期:2001-02-19 出版日期:2001-03-15 发布日期:2001-03-15
通讯作者: 徐萍*

Parallel Synthesis ofα-Acylamino Amide Library by Ugi four-component Condensation Reaction

Xu Ping^*, Lin Wenwei, Zhang Ting, Hu Xinge, Zou Xiaomin

1. Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University, Beijing 100083;
2. Department of Pharmacy, Yichang Medical School, Yichang 443000

Received:2000-11-28 Revised:2001-02-19 Online:2001-03-15 Published:2001-03-15
Contact: Xu Ping*

摘要/Abstract

摘要： Ugi-4CC四组份缩合反应是基于异腈的MCR's (多组份缩合反应)之中一类, 它以异腈、羧酸、醛、胺为原料, 可经一罐反应缩合生成由四种起始物共同组成的产物。此反应充分利用异腈的特性, 通过使用不同的反应物, 可用于合成不同结构骨架的系列化合物。本文合成了两种异腈,并进行了一系列Ugi反应以改进反应条件。

关键词: 多组份反应, 异腈, Ugi反应, 缩合条件

Abstract: Ugi-4CC(four-component condensation) reaction is one of isonitrile-based MCR’s (multi-component reactions), which is started with an amine, an aldehyde, a carboxylic acid and an isocyanide, after one-pot reaction to produce a compound composed of the whole four starting materials. The reaction makes full use of the specialty of isonitrile and can be used to build a series of compounds with different structural skeletons by using diverse inputs. In our work, two kinds of isonitriles were synthesized and a parallel synthesis of an α-acylamino amide library was performed to modify the Ugi reaction conditions.

Key words: MCR's multi-component reactions, Isonitrile, Ugi-4CC reaction, Condensation condition

Supporting: ^*Supported by the National Natural Science Foundation of China (39800186) and the National Major Program for Basic Research Development (973 project) from the Ministry of Science and Technology of China (G1998051114).
E-mail: pingxuzh@public.bta.net.cn

徐萍^*, 林文卫, 张婷, 胡兴娥, 邹晓民. 经Ugi四组份缩合反应进行α-氨酰基酰胺类化学库的平行合成[J]. .

Xu Ping^*, Lin Wenwei, Zhang Ting, Hu Xinge, Zou Xiaomin . Parallel Synthesis ofα-Acylamino Amide Library by Ugi four-component Condensation Reaction[J]. .

[1]	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]. , 2004, 13(4): 238-241.
[2]	王文浩, 张婷, 徐萍^*. Ugi四组分缩合反应合成肽核酸单体[J]. , 2003, 12(2): 66-70.