手性双环吡嗪酮的简洁合成作为约束性肽模拟砌块。

Concise synthesis of an enantiopure bicyclic pyrazinone as constrained peptidomimetic building block.

机构信息

CNRS UMR COBRA, INSA et Université de Rouen, FR 3038, Institut de Recherche en Chimie Organique Fine, Mont Saint-Aignan, France.

出版信息

Org Biomol Chem. 2012 Mar 14;10(10):2003-7. doi: 10.1039/c2ob06762e. Epub 2012 Feb 3.

DOI:10.1039/c2ob06762e

PMID:22302309

Abstract

A concise synthetic route has been developed for the preparation of a constrained peptidomimetic pyrazinone building block. From hydroxy-L-lysine, the desired pyrazinone is obtained in 43% overall yield (6 steps) via an efficient deprotection-double cyclization sequence.

摘要

已经开发出一种简洁的合成路线，用于制备约束性肽模拟吡嗪酮砌块。从羟基-L-赖氨酸出发，通过高效的脱保护-双环化序列，以 43%的总收率（6 步）得到所需的吡嗪酮。