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 ACIDUSING 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 is obtained by enzymatic hydrolysis of lovastatin acid or a salt thereof, by treating it with Clonostachys compactiuscula or mutant...

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Hauptverfasser: CONDER, MICHAEL J, STIEBER, ROBERT W, COVER, WILLIAM H, DABORA, REBECCA L, TEHLEWITZ, BOGDAN
Format: Patent
Sprache:eng ; fre
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Zusammenfassung: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 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.