首页> 外国专利> BIOSYNTHETIC PRODUCTION OF 6(R)-2-(8(S)-HYDROXY-2(S), 6(R)-DIMETHYL-1,2,6,7,8,8A(R)-HEXAHYDRONAPHTHYL)-ETHYL-4 (R)-HYDROXY-3,4,5,6-TETRAHYDRO-2H-PYRAN-2-ONE TRIOL ACID BY ENZYMATIC HYDROLYSIS OF LOVASTATIN ACID USING AN ENZYME DERIVED FROM__LONOSTACHYS COMPACTIUSCULA

BIOSYNTHETIC PRODUCTION OF 6(R)-2-(8(S)-HYDROXY-2(S), 6(R)-DIMETHYL-1,2,6,7,8,8A(R)-HEXAHYDRONAPHTHYL)-ETHYL-4 (R)-HYDROXY-3,4,5,6-TETRAHYDRO-2H-PYRAN-2-ONE TRIOL ACID BY ENZYMATIC HYDROLYSIS OF LOVASTATIN ACID USING AN ENZYME DERIVED FROM__LONOSTACHYS COMPACTIUSCULA

机译:6(R)-[2-(8(S)-HYDROXY-2(S),6(R)-二甲基-1,2,6,7,8,8,8A(R)-六亚乙基萘基)-乙基的生物合成洛伐他汀酸的酶促水解法合成紧凑型] -4(R)-羟基-3,4,5,6-四氢-2H-吡喃-2-一三醇酸

摘要

Biosynthetic production of6(R)-[2-(8(S)-hydroxy-2(S),6(R)-dimethyl-1,2,6,7,8,8a-(R)-hexahydronaphthyl)ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one triol acid is obtained byenzymatic hydrolysis of lovastatin acid or a saltthereof, by treating it with Clonostachyscompactiuscula or mutants thereof, or a hydrolasederived therefrom. The triol acid may be convertedin a straightforward manner to its lactone form; andboth are inhibitors of HMG-CoA reductase and thususeful as antihypercholesterolemic agents, and mayalso serve as intermediates for preparation of otherHMG-CoA reductase inhibitors.
机译:生物合成生产6(R)-[2-(8(S)-羟基-2(S),6(R)-二甲基-1,2,6,7,8,8a-((R)-六氢萘基)乙基] -4(R)-羟基-3,4,5,6-四氢-2H-吡喃-2-酮三醇酸是通过洛伐他汀酸或其盐的酶促水解通过用Clonostachys治疗致密菌或其突变体,或水解酶从中得出。三醇酸可被转化以其内酯形式的直接方式;和两者都是HMG-CoA还原酶的抑制剂,因此可用作抗高胆固醇血症药物,并可能也可以用作其他中间体的制备HMG-CoA还原酶抑制剂。

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