Applications of N-BOC-diamines for the solution phase synthesis of ketopiperazine libraries utilizing a Ugi/De-BOC/Cyclization (UDC) strategy

被引:61
作者
Hulme, C [1 ]
Peng, J [1 ]
Louridas, B [1 ]
Menard, P [1 ]
Krolikowski, P [1 ]
Kumar, NV [1 ]
机构
[1] Rhone Poulenc Rorer Cent Res, New Leads Discovery, Collegeville, PA 19426 USA
关键词
D O I
10.1016/S0040-4039(98)01770-5
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
This communication reveals a novel application of the 'so-called' convertible isonitrile for the solution phase generation of ketopiperazine libraries. Use of mono N-BOC diamines in the Ugi multicomponent reaction (MCR), followed by BOC removal and base treatment (a '3 step, 1-pot procedure') affords ketopiperazines in good yield. The generality of this procedure was further explored revealing novel routes to dihydroquinoxalinones and 1,4-benzodiazepines respectively (C) 1998 Elsevier Science Ltd. All rights reserved.
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收藏
页码:8047 / 8050
页数:4
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