Process for preparing statin precursor
AssigneeCentrient Pharmaceuticals Netherlands B.V.
InventorsBen De Lange, Karin Henderika Maria Bessembinder, Dennis Heemskerk
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Abstract
The present invention relates to a process for preparing a statin precursor, which process comprises a first reaction step, wherein a hydroxy-pyrimidine-carbonitrile is reacted with an organic sulfonyl halide to form the sulfonate-pyrimidine-carbonitrile; a second reaction step, wherein the sulfonate-pyrimidine-carbonitrile is reacted with N-methylmethane sulfonamide to form a pyrimidinyl-sulfonamide; and optionally a third reaction step, wherein the pyrimidinyl-sulfonamide is reacted with a reducing agent. All steps are conducted in toluene as the main solvent.
Claims20
A process for preparing the compound of formula (IV), the process comprising the steps of:
- (a) providing a starting mixture comprising the compound of formula (II) and toluene
- (b) a first reaction step, wherein the starting mixture is contacted with an organic sulfonyl halide and the resulting first reaction mixture is kept at a first temperature of below 110° C., thereby forming an intermediate mixture comprising the compound of formula (III)
- wherein R is an organic group having from 1 to 15 carbons;
- and
- (c) a second reaction step, wherein the intermediate mixture is contacted with N-methylmethane sulfonamide and the resulting second reaction mixture is kept at a second temperature, thereby forming a second mixture comprising the compound of formula (IV)
Dependencies are inferred from the claim text.