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N-甲酰基羟胺(反向/逆羟肟酸酯)的固相合成

Solid-phase synthesis of N-formylhydroxylamines (reverse/retro-hydroxamates).

作者信息

Price Steve, Osbourn Susan E

机构信息

Argenta Discovery Ltd., 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, UK.

出版信息

Org Lett. 2005 Aug 18;7(17):3761-3. doi: 10.1021/ol0513995.

DOI:10.1021/ol0513995
PMID:16092869
Abstract

N-Formylhydroxylamines, also known as reverse- or retro-hydroxamates, have become of significant interest in the recent past as inhibitors of metalloenzymes. Although solution-phase synthetic routes to such compounds have been reported, these are often lengthy and involve purification at each stage. Herein, novel three-step solid-phase synthetic approaches are described that enable libraries of such compounds to be produced in a convergent and efficient manner using commercially available starting materials. [reaction: see text]

摘要

N-甲酰基羟胺,也被称为反向或逆羟肟酸酯,近来作为金属酶抑制剂引起了极大的关注。尽管已经报道了此类化合物的溶液相合成路线,但这些路线通常冗长,且每个阶段都需要纯化。本文描述了新颖的三步固相合成方法,该方法能够使用市售起始原料以汇聚且高效的方式制备此类化合物的文库。[反应:见正文]

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