首页> 外国专利> ENANTIOSELECTIVE PRODUCTION METHOD OF OPTICALLY ACTIVE (S)-PROFEN FROM (R,S)-PROFEN RACEMATE BY USING CYCLODEXTRIN DERIVATIVE AS CHIRAL SELECTOR WITH HIGH PRODUCTION YIELD

ENANTIOSELECTIVE PRODUCTION METHOD OF OPTICALLY ACTIVE (S)-PROFEN FROM (R,S)-PROFEN RACEMATE BY USING CYCLODEXTRIN DERIVATIVE AS CHIRAL SELECTOR WITH HIGH PRODUCTION YIELD

机译:以环糊精衍生物为高产手性选择剂从(R,S)-脯氨酸的光学活性(S)-脯氨酸的对映异构生产方法

摘要

PURPOSE: An enantioselective production method of optically active (S)-profen from (R,S)-profen racemate using a cyclodextrin derivative as a chiral selector is provided, thereby improving the productivity of (S)-profen, easily recovering and recycling cyclodextrin and an enzyme, and simplifying the production process. CONSTITUTION: The enantioselective production method of optically active (S)-profen from (R,S)-profen racemate comprises adding cyclodextrin or its derivative as a chiral selector to various (R,S)-profen racemate such as ibuprofen, ketoprofen, naproxen, carprofen, fenoprofen, flurbiprofen, loxoprofen and suprofen; and reacting them in the presence of an enzyme such as lipase or esterase to form (S)-profen ester and a selective intermediate inclusion complex, wherein the chiral selector is alpha-cyclodextrin, beta-cyclodextrin, gamma-cyclodextrin, methyl-beta-cyclodextrin, dimethyl-beta-cyclodextrin, trimethyl-beta-cyclodextrin, randomly methylated-beta-cyclodextrin, hydroxypropyl-beta-cyclodextrin, hydroxypropyl-gamma-cyclodextrin, acetyl-beta-cyclodextrin, acetyl-gamma-cyclodextrin, triacetyl-beta-cyclodextrin, peracetyl-beta-cyclodextrin, peracetyl-gamma-cyclodextrin, or carboxylmethyl-beta-cyclodextrin.
机译:目的:提供一种使用环糊精衍生物作为手性选择剂从(R,S)-脯氨酸外消旋体制备旋光活性(S)-profen的对映选择性的方法,从而提高了(S)-profen的生产率,易于回收和再循环环糊精和酶,并简化了生产过程。组成:从(R,S)-脯氨酸外消旋体生产旋光性(S)-profen的对映选择性方法包括将环糊精或其衍生物作为手性选择剂添加到各种(R,S)-profen外消旋体如布洛芬,酮洛芬,萘普生,卡洛芬,非诺洛芬,氟比洛芬,洛索洛芬和舒洛芬;使它们在酶如脂肪酶或酯酶的存在下反应形成(S)-脯氨酸酯和选择性中间包合物,其中手性选择剂是α-环糊精,β-环糊精,γ-环糊精,甲基-β-环糊精,二甲基-β-环糊精,三甲基-β-环糊精,无规甲基化的β-环糊精,羟丙基-β-环糊精,羟丙基-γ-环糊精,乙酰基-β-环糊精,乙酰基-γ-环糊精,三乙酰基-β-环糊精,全乙酰基-β-环糊精,过乙酰基-γ-环糊精或羧甲基-β-环糊精。

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