Process of lactonization in the preparation of statins

Details Process of lactonization in the preparation of statins Process of lactonization in the preparation of statins

1998-04-22

1999-06-29

Owens, Amelia

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D30930

Patent

active

059170581

ABSTRACT:
An improved process of lactonization in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises treating the open ring hydroxy acid form of the statins with an excess of acetic acid and in the absence of a strong acid catalyst under mild heating conditions (e.g., ambient to 55.degree. C.), and adding an anti-solvent to the reaction mixture, thereby causing the statins in lactone form to crystalize from the reaction mixture. The acetic acid serves as both a solvent and a catalyst for the lactonization reaction.

REFERENCES:
patent: 4820850 (1989-04-01), Verhoeven et al.
patent: 4916239 (1990-04-01), Treiber

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