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. |
申请人 |
MERCK & CO., INC., RAHWAY, N.J., US |
发明人 |
CONDER, MICHAEL J., HARRISONBURG, VA 22801, US;COVER, WILLIAM H., MCGAHEYSVILLE, VA 22840, US;DABORA, REBECCA L., ANDOVER, MA 01810, US;STIEBER, ROBERT W., HARRISONBURG, VA 22801, US;TEHLEWITZ, BOGDAN, MCGAHEYSVILLE, VA 22840, US |