BIOSYNTHETIC METHOD OF MANUFACTURING 6(R)-(2-(8(S)- HYDROXY-2-(S),6(R)-DIMETHYL-1,2,6,7,8,8A(R)-HEXAHYDRO- NAPHTHYL)-ETHYL)4(R)-HYDROXY-3,4,5,6-TETRAHYDRO-2H-PYRAN- 2-ONE TRIOL ACID BY ENZYMATIC HYDROLYSIS OF ROBASTATINIC ACID BY USING ENZYME OBTAINED FROM CHRONOSTAKIS COMPACTIUSCULA

摘要

Biosynthetic production of 6(R)-[2-(8(S)-hydroxy-2(S),6(R)-dimethyl-1,2,6,7,8,8a(R)-hexahydronaph thyl)ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-on e triol acid is obtained by enzymatic hydrolysis of lovastatin acid or a salt thereof, by treating it with Clonostachys compactiuscula or mutants thereof, or a hydrolase derived therefrom. The triol acid may be converted in a straightforward manner to its lactone form; and both are inhibitors of HMG-CoA reductase and thus useful as antihypercholesterolemic agents, and may also serve as intermediates for preparation of other HMG-CoA reductase inhibitors.