| 摘要 |
1377308 Substituted 5-phenoxy and 5-thiophenoxy-2-(1H)-pyrimidinones PFIZER Inc 18 Feb 1972 [29 Oct 1971] 7748/72 Heading C2C Novel compounds of the Formula I: wherein R is hydrogen or methyl, R 1 is oxygen or sulphur, R 2 is hydrogen, halogen or methyl and R 3 is hydrogen, methyl, chloro or trifluoromethyl and pharmaceutically acceptable salts thereof may be prepared by reacting a compound wherein R 6 and R 7 are C 1-3 alkyl groups, with a reagent prepared from ethanol, sodium and urea and if necessary reacting the product with an alkali metal or alkaline earth metal salt and hot methyl iodide to introduce the methyl group at R. 2 - (p - Chlorophenoxy) - 3 - dimethylaminoacrolein may be prepared by reacting potassium p-chlorophenolate, prepared in situ, with chloroacetaldehyde diethylacetal to yield pchlorophenoxyacetaldehyde diethyl acetal which on reaction with dimethyl formamide in the presence of phosphorus oxychloride cyclizes to the required intermediate. Pharmaceutical compositions of the compound I with the usual excipients show bronchodilatory activity and inhibit gastric acid secretion when administered orally, parenterally or by inhalation. |
