手性非外消旋α-硼基异氰化物的简便合成。
Straightforward synthesis of chiral non-racemic α-boryl isocyanides.
机构信息
Department of Life Sciences, Università degli Studi di Modena e Reggio Emilia, via G. Campi 103, 41125, Modena, Italy.
出版信息
Org Biomol Chem. 2021 Aug 5;19(30):6687-6691. doi: 10.1039/d1ob00616a.
PMID:34286797
Abstract
A straightforward concise synthesis of chiral non-racemic aliphatic α-boryl isocyanides, relay intermediates for boron-based bioactive molecules in multicomponent reactions, is presented. The short synthetic sequence comprises as key steps copper-catalysed asymmetric borylation of imines, simultaneous nitrogen formylation/boron-protecting group interconversion and the final formamide dehydration reaction.
摘要
本文提出了一种直截了当的简洁方法，用于合成手性非外消旋脂肪族 α-硼基异氰化物，这是多组分反应中基于硼的生物活性分子的中继中间体。该简短的合成序列包括关键步骤：铜催化的亚胺不对称硼化、同时进行氮甲酰化/硼保护基相互转化以及最终的甲酰胺脱水反应。
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