6-Substituted-5H-pyrrolo[2,3-b]pyrazines via palladium-catalyzed heteroannulation from N-(3-chloropyrazin-2-yl)methanesulfonamide and alkynes

被引:25
作者
Hopkins, CR [1 ]
Collar, N [1 ]
机构
[1] Aventis Pharmaceut, Drug Innovat & Approval, Dept Med Chem, Bridgewater, NJ 08807 USA
关键词
6-substituted-5H-pyrrolo[2,3-b]pyrazine; heteroannulation; palladium; cyclization;
D O I
10.1016/j.tetlet.2004.08.155
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We herein report the efficient and convenient synthesis of 6-substituted-5H-pyrrolo[2,3-b]pyrazines. The reaction is a palladium-catalyzed heteroannulation process followed by deprotection to yield the desired pyrrolo[2,3-b]pyrazine substrates. The reaction starts with readily accessible N-(3-chloropyrazin-2-yl)-methanesulfonamide and commercially available terminal alkynes and works with aryl- and alkylalkynes. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:8087 / 8090
页数:4
相关论文
共 70 条
[11]  
Deprets S. D.
[12]  
Edlin C.
[13]  
Gardner C. J.
[14]  
Kominos D.
[15]  
Pedgrift B. L.
[16]  
Halley F.
[17]  
Gillepsy T. A.
[18]  
Edwards M.
[19]  
Clerc F. F.
[20]  
Nemecek C.