PROCESS FOR PREPARING NOVEL PYRIMIDINONE DERIVATIVES

1377720 Phenoxy hydroxy pyrimidines PFIZER Inc 18 Feb 1972 [29 Oct 1971] 50053/73 Divided out of 1377308 Heading C2C Novel compounds of the Formula I and pharmaceutically acceptable salts thereof wherein R 4 is hydrogen, halogen, C 1-3 alkyl, methoxy or carboxy and R 5 is hydrogen, chloro or methyl may be prepared by reacting the sodium salt of a compound II where R 6 is C 1-3 alkyl with ethanol, thiourea and sodium methoxide, desulphurizing the thiouracil formed and acidifying the product to yield I. The sodium salt of ethyl α-(p-chlorophenoxy)- #-hydroxyacrylate may be prepared by reacting ethyl chloroacetate with p-chlorophenol in the presence of sodium ethoxide to yield ethyl p-chlorophenoxyacetate which yields the required compound or reaction with methyl formate and sodium sand. Pharmaceutical compositions of the compound I with the usual excipients show bronchodilatory activity when administered orally, parenterally or by inhalation.