Tetrahedron Letters

Solid-phase synthesis of N, N′-substituted acylguanidines

DS Dodd, Y Zhao

文献索引：Dodd, Dharmpal S.; Zhao, Yufen Tetrahedron Letters, 2001 , vol. 42, # 7 p. 1259 - 1262

全文：HTML全文

被引用次数: 17

摘要

An efficient method for the solid-phase synthesis of N, N′-substituted acylguanidines is presented. The key-step involves the N-acylation of resin immobilized S-methylisothiourea with a variety of carboxylic acids using PyAOP as the coupling agent. The resulting resin bound N-acyl-derivatives are reacted with a host of amines and the N-acyl, N′-alkyl (aryl) guanidines liberated from the resin upon exposure to TFA.