Two-step solution-phase synthesis of novel benzimidazoles utilizing a UDC (Ugi/de-Boc/cyclize) strategy
Two-step solution-phase synthesis of novel benzimidazoles utilizing a UDC (Ugi/de-Boc/cyclize) strategy
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DOI：
10.1016/s0040-4039(01)00919-4
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发表时间：
2001-07-23
影响因子：
1.8
通讯作者：
Hulme, C
中科院分区：
文献类型：
--
作者：
Tempest, P;Ma, V;Hulme, C
揭示了一系列生物相关的苯并咪唑类化合物的新的两步液相合成方法。通过单Boc保护的邻苯二胺和支持的UGI试剂的缩合，以极高的产率进行转化。随后的酸处理和蒸发以很好到很好的产率提供了苯并咪唑。所描述的方案代表了一种用于快速生成苯并咪唑文库的极具吸引力的溶液相程序。(C)2001爱思唯尔科学有限公司。保留所有权利。
The novel solution-phase synthesis of an array of biologically relevant benzimidazoles in a simple two-step procedure is revealed. Transformations are carried out in excellent yield by condensation of mono-Boc protected ortho-phenylene diamine and supporting Ugi reagents. Subsequent acid treatment and evaporation affords benzimidazoles in good to excellent yield. The described protocol represents a highly attractive solution-phase procedure for the rapid generation of benzimidazole libraries. (C) 2001 Elsevier Science Ltd. All rights reserved.