IMPROVED METHOD FOR LACTONIZATION IN PREPARING STATINS Russian patent published in 2003 - IPC

Abstract RU 2214407 C2

FIELD: organic chemistry, chemical technology, biochemistry, medicine. SUBSTANCE: invention relates to the improved method for lactonization in preparing statins, for example, inhibitors of activity of HMG-CoA-reductase: lovastatin and simvastatin. In part, invention relates to method for preparing compound of the formula (I) wherein R represents radical of the formula (III) wherein R1 represents hydrogen atom or CH3,. Method involves the following stages: (a) treatment of compound of the formula (II) NH4 wherein Z represents hydrogen atom, metal cation or ; R is given above. Treatment is carried out with weak organic acid in the absence of strong acid as a catalyst and water at temperature below 55 C; (b) addition of anti-solvent that causes precipitation of compound of the formula (I) as crystalline product. Proposed method without using strong corrosion acids and rigid heating conditions allows preparing the end product with high purity above 98% and high yield above 98%. EFFECT: improved preparing method, enhanced purity and yield. 9 cl

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RU 2 214 407 C2

Authors

Kumar Jatendra

Taper Radzhesh Kumar

Kumar S. M. Dilip

Kkhanna Dzhag Mokhan

Dates

2003-10-20Published

1998-12-09Filed