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用于 GABA 类药物直接可持续合成的多相有机-无机杂化催化剂。

Multisite organic-inorganic hybrid catalysts for the direct sustainable synthesis of GABAergic drugs.

机构信息

Instituto de Tecnología Química, UPV-CSIC, Universidad Politécnica de Valencia, Avenida de los Naranjos s/n, 46022 Valencia (Spain) http://itq.upv-csic.es/en/

出版信息

Angew Chem Int Ed Engl. 2014 Aug 11;53(33):8687-90. doi: 10.1002/anie.201403049. Epub 2014 Jun 18.

Abstract

Multisite organic-inorganic hybrid catalysts have been prepared and applied in a new general, practical, and sustainable synthetic procedure toward industrially relevant GABA derivatives. The domino sequence is composed of seven chemical transformations which are performed in two one-pot reactions. The method produces both enantiomeric forms of the product in high enantiopurity as well as the racemate in good yields after a single column purification step. This protocol highlights major process intensification, catalyst recyclability, and low waste generation.

摘要

多相有机-无机杂化催化剂已被制备并应用于一种新的通用、实用且可持续的工业相关 GABA 衍生物的合成方法中。该串联反应由七个化学反应组成,在两个一锅反应中进行。该方法在单一柱纯化步骤后,以高对映体纯度和良好收率得到产物的对映异构体以及外消旋体。该方案突出了主要的过程强化、催化剂的可回收性和低废物生成。

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