Facile synthesis of substituted 2,3,4,7-tetrahydro-1H-azepines via ring-closing metathesis

摘要

A highly efficient synthesis based on inexpensive and readily available starting material towards the pharmacologically interesting class Of Substituted 2,3,4,7-tetrahydro-1H-azepines via a ring-closing metathesis (RCM) approach employing Grubbs catalysts 1 and 2 is described. The influence of the substituents R-1 and R-2 on the outcome of the RCM reaction is discussed. The seemingly first example of an RCM approach towards seven-membered azacycles bearing a substituent at the alkene moiety Utilizing Grubbs catalyst 1 is presented. (c) 2005 Elsevier Ltd. All rights reserved.