The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jun. 29, 1993

Filed:

Feb. 07, 1992
Applicant:
Inventors:

Michael J Conder, Harrisonburg, VA (US);

Steven J Cianciosi, Harrisonburg, VA (US);

William H Cover, Lansdale, PA (US);

Rebecca L Dabora, Andover, MA (US);

Eric T Pisk, Harrisonburg, VA (US);

Robert W Stieber, Harrisonburg, VA (US);

Bogdan Tehlewitz, McGaheysville, VA (US);

Gregory L Tewalt, Shenandoah, VA (US);

Assignee:

Merck & Co., Inc., Rahway, NJ (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C12P / ; C12P / ; C12N / ; C07D / ;
U.S. Cl.
CPC ...
435125 ; 435117 ; 435 41 ; 435183 ; 435195 ; 549292 ;
Abstract

Biosynthetic production of 7-[1',2',6',-7',8',8a'(R)-hexahydro-2'(S),6'(R)-dimethyl-8'(S)-hydroxy-1'( S)-naphthyl]-3(R),5(R)-dihydroxyheptanoic acid, 'triol acid', is accomplished by enzymatic hydrolysis of lovastatin acid or a salt thereof, by treating it with Clonostachys compactiuscula ATCC 38009 or ATCC 74178, or mutants thereof, or a cell-free extract derived therefrom, or a hydrolase derived therefrom. The triol acid and its lactone form are both inhibitors of HMG-CoA reductase and thus useful as anti-hypercholesterolemic agents, and may also serve as intermediates for preparation of other HMG-CoA reductase inhibitors. Also, in the synthesis of simvastatin by direct methylation of lovastatin, selective hydrolysis of residual lovastatin salt by treatment with Clonostachys compactiuscula ATCC 38009 or ATCC 74178 or mutants thereof or a cell-free extract derived therefrom, or a hydrolase derived therefrom yields the 'triol' salt which can be easily separated from simvastatin.


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