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

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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.