The solution phase synthesis of diketopiperazine libraries via the Ugi reaction: Novel application of Armstrong's convertible isonitrile.

被引:109
|
作者
Hulme, C [1 ]
Morrissette, MM [1 ]
Volz, FA [1 ]
Burns, CJ [1 ]
机构
[1] Rhone Poulenc Rorer Cent Res, Collegeville, PA 19426 USA
关键词
D O I
10.1016/S0040-4039(97)10795-X
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
This communication describes the generation of high-yielding solution phase diketopiperazine libraries via a '3-step, 1-pot' procedure, employing the Ugi multi-component reaction (MCR), followed by BOC deprotection and cyclization to diketopiperazine (DKP). Exploitation of Armstrong's convertible isonitrile in the Ugi reaction utilising an 'internal nucleophile' approach for diketopiperazine formation is presented. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1113 / 1116
页数:4
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