C - Chemistry – Metallurgy – 12 – P
Patent
C - Chemistry, Metallurgy
12
P
C12P 17/06 (2006.01) C07C 59/46 (2006.01) C07C 69/30 (2006.01) C07D 309/30 (2006.01) C12P 7/42 (2006.01) C12P 13/00 (2006.01) C12P 17/14 (2006.01)
Patent
CA 2129661
In the synthesis of simvastatin by direct methylation of lovastatin, selective hydrolysis of residual lovastatin, lovastatin acid or a salt thereof by treatment with a bacterium or fungus capable of hydrolyzing the 2-methyl-butyryloxy side chain or a mutant of such microbe or a cell-free extract derived therefrom, or a hydrolase derived therefrom yields 7-[1',2',6',7',8',8a'(R)-hexahydro- 2'(S),6'(R)-dimethyl-8'(S)-hydroxy-1'(S)naphthyl]-3(R),5(R)-dihydroxy- heptanoic acid, the triol acid, or triol salt which can be easily separated from simvastatin, either before or after lactonization to the lactone form. This process produces simvastatin of high yield and purity.
Cianciosi Steven J.
Conder Michael J.
Pisk Eric T.
Tewalt Gregory L.
Merck & Co. Inc.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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