Chemoenzymatic Dynamic Kinetic Resolution of Amines in Fully Continuous-Flow Mode
作者:Emese Farkas、Márk Oláh、Attila Földi、János Kóti、János Éles、József Nagy、Cristian Andrei Gal、Csaba Paizs、Gábor Hornyánszky、László Poppe
DOI:10.1021/acs.orglett.8b03676
日期:2018.12.21
In this study, lipase-mediated dynamic kinetic resolution (DKR) of various benzylic amines (1a–g) is presented which is realized in a so far unprecedented fully continuous-flow system. The DKR process applying sol–gel immobilized lipase B from Candida antarctica as biocatalyst, palladium on 3-aminopropyl-functionalized silica as racemization catalyst, isopropyl 2-ethoxyacetate as acylating agent, ammonium
在这项研究中,提出了脂肪酶介导的各种苄基胺(1a – g)的动态动力学拆分(DKR),这是迄今为止前所未有的完全连续流动的系统所实现的。DKR工艺采用南极假丝酵母的溶胶-凝胶固定化脂肪酶B作为生物催化剂,3-氨基丙基官能化二氧化硅上的钯作为外消旋催化剂,2-乙氧基乙酸异丙酯作为酰化剂,甲酸铵作为氢和氮源,以及2-甲基-2在调节的压力下,以-丁醇为溶剂,以中等至良好的收率提供了所需的产物,并具有优异的对映体过量。