Patent ID: 6121447
Filing Date: 2000-09-19
Classification: A61P,C07D

Abstract:
A process for the manufacturing 4-tert.butyl-N-6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(pyrimidin-2-y l)-pyrimidin-4-yl-benzenesulphonamide, which comprises:a) manufacturing 2-cyanopyrimidine by reacting 2-chloropyrimidine with an alkali cyanide in the presence of 1-azabicyclo[2,2,2]octane or 1,4-diazabicyclo[2,2,2]octane;b) converting the 2-cyanopyrimidine by means of NH.sub.3 /NH.sub.4 Cl in a sodium methanolate/methanol solution into pyrimidin-2-carboxamidine hydrochloride;c) converting the product obtained in (b) in the presence of sodium methanol ate with diethyl (o-methoxy-phenoxy-malonate) into rac-5-(2-methoxy-phenoxy)-2-pyrimidin-2-yl-tetrahydro-pyrimidin-4,6-dione;d) reacting the product obtained in (c) with N,N-diisopropyl-N-ethylamine and phosphorus pentachloride to give 4,6-dichloro-5-(2-methoxy-phenoxy)-2,2'-bipyrimidine;e) reacting the product obtained in d) with p-tert.butylbenzenesulphonamide to give 4-tert.butyl-N-6-chloro-5-[2-(2-methoxy-phenoxy)-2-(pyrimidin-2-yl)-pyrimi din-4-yl]-benzenesulphonamide; andf) reacting the product obtained in (e) with sodium ethylene glycolate to give 4-tert.butyl-N-6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(pyrimidin-2-y l)-pyrimidin-4-yl-benzenesulphonamide.