Synthetic study on biological active natural products by means of Ugi reaction

UGI四组分缩合反应(UGI 4CC)由于在温和的条件下通过简单的实验过程提供了各种α-氨基酰胺衍生物而得到了广泛的应用。最近，我们开发了一种新型的异腈，它不仅具有无味性质，而且还具有易于转化的乌吉加合物的C-端酰胺。本研究利用我们的新型异腈，通过乌吉反应，合成了对M受体具有亚型选择性亲和力的高效免疫抑制剂FR901483和TAN1251A。

The Ugi four-component condensation (Ugi 4CC) has been widely employed since it provides various alfa-amino amide derivatives by a simple experimental procedure under mild conditions. Recently, we have been developed novel isonitrile, which possessed odorless nature as well as readily convertible C-terminal amide of Ugi adducts. In this research, total synthesis of potent immunosuppressant FR901483 and TAN1251A, which possessed the subtype selective affinity against the muscarinic receptors have been accomplished by means of Ugi reaction with utilizing our novel isonitrile.