MANUFACTURE OF ALPHA-(1-METHYLETHYL)-3,4- DIMETHOXYBENZENEACETONITRILE AND INTERMEDIATE THEREFOR

摘要

New process for the synthesis of the alpha -(1-methylethyl)-3,4-dimethoxyacetonitrile of formula CHEM intermediate in the synthesis of the drug internationally known as verapamil. The process starts from the isobutyryl-3,4-dimethoxybenzene of formula CHEM which, by means of the Darzens condensation, gives an epoxyester which, by alkaline hydrolysis and subsequent decarboxylation, gives the alpha -(1-methylethyl)-3,4-dimethoxybenzeneacetaldehyde. This product is reacted with hydroxylamine so obtaining the corresponding oxime that, by dehydratation, gives the nitrile of formula I.