| 摘要 |
1373536 4-Hydroxy-6-arylpyrimidines PFIZER Inc 4 Oct 1971 [5 Oct 1970] 38316/73 Divided out of 1373535 Heading C2C Novel 4-hydroxy-6-arylpyrimidines of the general formula wherein R 3 is a hydrogen atom or a C 1-3 alkyl group and Ar is a phenyl group (provided that R 3 is an ethyl group); a phenyl group monosubstituted by a fluorine, chlorine or bromine atom or a methyl, methoxy, hydroxy, trifluoromethyl, carboxy, cyano, nitro, di-C 1-3 alkylamino, amino or C 1-4 acylamino group; a 3,4-dimethoxyphenyl group; a pyridyl, thienyl or furyl group optionally monosubstituted by a C 1-4 acylamino group; or a naphthyl, 2- or 3-indolyl, 2- or 3-benzothienyl or 2- or 3-benzofuryl group, are prepared (a) by treatment of an ethyl 2-R 3 - 3-Ar-3-amino-acrylate with formamide in the presence of an alkali metal alkoxide; and (b) by reaction of an ethylα-ArCO-α-R 3 -acetate with thiourea and treatment of the resulting 2- mercapto-4-hydroxy-5-R 3 -6-Ar-pyrimidine with Raney nickel in aqueous sodium hydroxide. Pharmaceutical compositions having smooth muslce relaxant activity comprise, as active ingredient, 4-hydroxy-5-ethyl-6-phenylpyrimidine, together with a pharmaceutical carrier.
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