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

被引:19
作者
Brass, S [1 ]
Gerber, HD [1 ]
Dörr, S [1 ]
Diederich, WE [1 ]
机构
[1] Univ Marburg, Inst Pharmazeut Chem, Fachbereich Pharm, D-35037 Marburg, Germany
关键词
azacycles; lactames; beta-amino ester;
D O I
10.1016/j.tet.2005.11.049
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
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.
引用
收藏
页码:1777 / 1786
页数:10
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