Microwave-assisted direct amination:: Rapid access to multi-functionalized N6-substituted adenosines

被引:14
作者
Ashton, Trent D. [1 ]
Scammells, Peter J. [1 ]
机构
[1] Monash Univ, Victorian Coll Pharm, Dept Med Chem, Parkville, Vic 3052, Australia
关键词
D O I
10.1071/CH07340
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Analogues of adenosine have a range of interesting biological activities and potential therapeutic applications. A method for the efficient preparation of highly functionalized N-6-substituted adenosines has been developed from the corresponding tert-butyldimethylsilyl-protected inosine. The key step in this procedure is a microwave-assisted amination reaction between an appropriately substituted inosine and an amine in the presence of PyBroP. High yields of desired N6-substituted adenosines were achieved with hindered amines and the reaction was also found to accommodate a range of substituents on the inosine precursor.
引用
收藏
页码:49 / 58
页数:10
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