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methylopyl sp. and use thereof in the preparation of selective resolution of (s) -alpha-ethyl-2-oxo-1-pyrrolidine acetate

机译:甲基鸦片及其在制备(s)-α-乙基-2-氧-1-吡咯烷乙酸盐的选择性拆分中的用途

摘要

The present invention describes methyl spila sp. and use thereof in the preparation of selective resolution of (s) -alpha-ethyl-2-oxo-1-pyrrolidine acetate. methylopyl sp. which produces enzymes is subjected to cell immobilization, and is then applied to the biological resolution of an acetic acid (r, s) -alpha-ethyl-2-oxo-1-pyrrolidine ethyl ester racemate to prepare (s) ethyl ester High optical purity acetic) alpha-2-oxo-1-pyrrolidine, which is further subjected to a hydrolysis reaction to obtain (s) -alpha-ethyl-2-oxo-1-pyrrolidine acetate. The present invention achieves a high conversion yield of up to 50.0% or more, good stereoselectivity, and an enantiomeric excess value of (s) -alpha-ethyl-2-oxo-1-pyrrolidine acetic acid ethyl ester. less than 99.5; catalytic efficiency is high; The concentration of racemic substrate in the resolution reaction is up to 500 g / l, the reaction time does not exceed 15 hours, the number of reuse times of immobilized cells is not lower than 35, and thus the present invention is convenient. For industrial production, it is simple in downstream separation and produces little environmental pollution.
机译:本发明描述了甲基spila sp。及其在制备(s)-α-乙基-2-氧代-1-吡咯烷乙酸酯的选择性拆分中的用途。甲基鸦片产生酶的酶进行细胞固定,然后应用于乙酸(r,s)-α-乙基-2-氧代-1-吡咯烷乙酯外消旋体的生物拆分,以制备(s)乙酯纯度的乙酸)α-2-氧代-1-吡咯烷,将其进一步进行水解反应以获得(α)-α-乙基-2-氧代-1-吡咯烷乙酸盐。本发明实现了高达50.0%或更高的高转化率,良好的立体选择性和(s)-α-乙基-2-氧代-1-吡咯烷乙酸乙酯的对映体过量值。小于99.5;催化效率高;拆分反应中外消旋底物的浓度最高为500 g / l,反应时间不超过15小时,固定化细胞的重用次数不低于35,因此本发明是方便的。对于工业生产,它在下游分离中很简单,并且几乎不污染环境。

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