US 6,649,775 B2 · Process of lactonization in the preparation of statins

Abstract

The present invention relates to a process for preparing lovastatin and simvastatin which comprises (1) performing step of a lactonization of mevinic acid and analog thereof compounds in the presence of a dehydrating agent and without an acid catalyst under nitrogen sweep; and then (2) making step of crystals at a high temperature. In the process of the present invention, lovastatin and simvastatin highly purified can be produced in a high yield and especially, heterodimers formed as a by-product can be reduced in an amount remarkably. Therefore, the process of the present invention is convenient and economical.

Claims6

Dependent claims

A method for preparing a compound of Formula 1

wherein R is a radical of Formula 3
wherein R1 is H or CH3,
which comprises the steps of:
lactonizing a compound of Formula 2
wherein Z is hydrogen, ammonium or metal cation, in the presence of a dehydrating agent under nitrogen sweep and without acid catalyst;
and crystallizing the obtained lactone product in a solvent.

3 more elements

Dependencies are inferred from the claim text.

Process of lactonization in the preparation of statins

Life of this patent

Process of lactonization in the preparation of statins

Life of this patent

Abstract

Claims6