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ENZYMATIC METHOD FOR PRODUCING 17-MONOESTERS OF CORTEXOLON AND / OR THEIR 9,11-DEHYDRO DERIVATIVES

机译:酶法生产皮质酮的17-单体和/或其9,11-脱水衍生物

摘要

1. A method of obtaining compounds of formula (I)! ! in which R represents a linear or branched aliphatic or aromatic chain containing from 1 to 10 carbon atoms, characterized in that the compound of formula II! ! in which R has the same meanings as above, are reacted with a compound of formula III! R'OH, (III)! In which R 'represents a linear aliphatic chain containing from 1 to 10 carbon atoms, in the presence of lipase from Candida. ! 2. The method of claim 1, wherein R is C1-C4 alkyl. ! 3. The method according to claim 1, in which R is selected from CH3, CH3CH2, CH3 (CH2) 2 or CH3 (CH2) 3. ! 4. The method according to claim 1, in which R 'is an aliphatic chain containing 1-8 carbon atoms. ! 5. The method according to claim 1, characterized in that it is carried out in the presence of an organic solvent, preferably aprotic. ! 6. The method according to claim 5, wherein said solvent is selected from toluene, acetonitrile, tetrahydrofuran, dichloromethane and / or chloroform. ! 7. The method according to claim 1, wherein said compound of formula II is present in an amount of from about 0.01 to 0.15 mol / L. ! 8. The method according to claim 7, in which the specified compound of formula II is present in an amount of 0.025 mol / L. ! 9. The method according to claim 1, wherein said compound of formula III is selected from methanol, ethanol, butanol and / or octanol. ! 10. The method according to claim 1, wherein said compound of formula III is present in an amount of from about 0.5 to about 50 moles per mole of the starting substrate. ! 11. The method according to claim 1, wherein said compound of formula III is present in an amount of 5 moles per mole of the starting substrate. ! 12. The method according to claim 1, in which the specified lipase from Candida selected from CCL and CALB. ! 13. The method according to claim 1, wherein said lipase from
机译:1.一种获得式(I)化合物的方法! !其中R代表含有1至10个碳原子的直链或支链脂族或芳族链,其特征在于式II的化合物! !其中R具有与上述相同的含义,与式III的化合物反应! R'OH,(III)!其中R′代表在来自假丝酵母的脂肪酶存在下的含有1至10个碳原子的线性脂族链。 ! 2.权利要求1的方法,其中R是C1-C4烷基。 ! 3.根据权利要求1所述的方法,其中,R选自CH 3,CH 3 CH 2,CH 3(CH 2)2或CH 3(CH 2)3。 4.根据权利要求1的方法,其中R'是含有1-8个碳原子的脂族链。 ! 5.根据权利要求1的方法,其特征在于它是在有机溶剂,优选非质子的存在下进行的。 ! 6.根据权利要求5的方法,其中所述溶剂选自甲苯,乙腈,四氢呋喃,二氯甲烷和/或氯仿。 ! 7.根据权利要求1的方法,其中所述式II化合物的存在量为约0.01至0.15mol / L。 8.根据权利要求7的方法,其中特定的式II化合物的存在量为0.025mol / L。 9.根据权利要求1的方法,其中所述式III的化合物选自甲醇,乙醇,丁醇和/或辛醇。 ! 10.根据权利要求1的方法,其中所述式III化合物的存在量为每摩尔起始底物约0.5至约50摩尔。 ! 11.根据权利要求1的方法,其中所述式III的化合物以每摩尔起始底物5摩尔的量存在。 ! 12.根据权利要求1的方法,其中来自念珠菌的特定脂肪酶选自CCL和CALB。 ! 13.根据权利要求1的方法,其中所述脂肪酶来自

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