Novel safety-catch linker and its application with a Ugi/De-BOC/cyclization (UDC) strategy to access carboxylic acids, 1,4-benzodiazepines, diketopiperazines, ketopiperazines and dihydroquinoxalinones

被引：113

作者：

Hulme, C ^{[1
]}

Peng, J ^{[1
]}

Morton, G ^{[1
]}

Salvino, JM ^{[1
]}

Herpin, T ^{[1
]}

Labaudiniere, R ^{[1
]}

机构：

[1] Rhone Poulenc Rorer Cent Res, Lead Discovery, Collegeville, PA 19426 USA

来源：

TETRAHEDRON LETTERS | 1998年 / 39卷 / 40期

关键词：

D O I：

10.1016/S0040-4039(98)01593-7

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

This communication reveals the synthesis and application of a novel resin bound isonitrile. The resin is an example of a novel safety-catch linker which upon BOG-activation can be resin cleaved with a variety of nucleophiles. Use of this polymer supported isonitrile in the Ugi multi-component reaction (MCR), followed by resin clipping and cyclization allows access to diverse arrays of 1,4-benzodiazepine-2,5-diones, diketopiperazines and ketopiperazines respectively. The methoxide safety-catch clipping strategy and subsequent solution phase cyclization offers similar advantages to a traceless linker. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：7227 / 7230

页数：4

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