首页> 外国专利> METHOD FOR PRODUCING STEROID DERIVATIVES BY REDUCING OXOSTEROID COMPOUNDS OR OXIDATION OF HYDROXYSTEROID COMPOUNDS USING A HYDROXYSTEROID DYHYDROGENASE

METHOD FOR PRODUCING STEROID DERIVATIVES BY REDUCING OXOSTEROID COMPOUNDS OR OXIDATION OF HYDROXYSTEROID COMPOUNDS USING A HYDROXYSTEROID DYHYDROGENASE

机译:通过减少羟基甾体化合物或使用羟基甾体二羟化酶氧化羟基甾体化合物来生产甾体衍生物的方法

摘要

1. The method of enantioselective enzymatic recovery of compounds having a steroid structure (ABCD), including one or more heteroatoms, one or more double bonds and / or aromatic link in the cyclic structure, and containing at least one oxo group in position 3, 7, 11, 12 or 17 of the steroidal cyclic system or in the α-position of any carbon residue on the steroid skeleton (= oxosteroid compound),! ! moreover, the oxosteroid compound is reduced with hydroxysteroid dehydrogenase in the presence of the cofactor NADH or NADPH, characterized in that! a) the oxosteroid compound is in the reaction mixture at a concentration of ≥50 g / l,! b) the oxidized cofactor NAD or NADP formed by hydroxysteroid dehydrogenase is continuously reduced via oxidation of a secondary alcohol of the general formula RXRYCHOH, where RX, RY are independently hydrogen, branched or unbranched C1-C8-alkyl, and Ctot ≥ 3, or via oxidation C4-C6-cycloalkanol, and! c) additional oxidoreductase / alcohol dehydrogenase is used to oxidize the secondary alcohol of the general formula RXRYCHOH or cycloalkanol. ! 2. The method according to claim 1, characterized in that the compound of general formula I is used as the oxosteroid compound! ! in which mean:! R1 is hydrogen, methyl group, hydroxy group or oxo group! R2 is hydrogen, methyl group, hydroxy group or oxo group! R3 is hydrogen, a hydroxy group, an oxo group or a methyl group,! R4 is hydrogen or a hydroxy group! R5 is hydrogen, the residue is -COR10, where R10 is an unsubstituted or hydroxy-substituted C1-C4-alkyl group or substituted or unsubstituted
机译:1.具有甾类结构(ABCD)的化合物的对映选择性酶促回收的方法,所述甾类结构包括一个或多个杂原子,环状结构中的一个或多个双键和/或芳族键,并且在3位上含有至少一个氧代基,类固醇循环系统的7、11、12或17或类固醇骨架(=氧类固醇化合物)上任何碳残基的α-位置! !而且,在辅助因子NADH或NADPH存在下,羟甾类化合物被羟甾类脱氢酶还原,其特征在于! a)反应混合物中的氧甾类化合物浓度≥50 g / l! b)由羟基类固醇脱氢酶形成的氧化的辅因子NAD或NADP通过通式RXRYCHOH的仲醇的氧化连续还原,其中RX,RY独立为氢,支链或直链C1-C8烷基且Ctot≥3,或通过氧化C4-C6-环烷醇, c)另外的氧化还原酶/醇脱氢酶用于氧化通式RXRYCHOH的仲醇或环烷醇。 ! 2.根据权利要求1的方法,其特征在于将通式I的化合物用作氧类固醇化合物! !其中的意思是:! R1是氢,甲基,羟基或氧代基! R 2是氢,甲基,羟基或氧代基! R 3是氢,羟基,氧代基或甲基,! R4是氢或羟基! R 5是氢,残基是-COR 10,其中R 10是未取代或羟基取代的C 1 -C 4烷基或取代或未取代的

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