| 摘要 |
1,270,120. Pyrimidine carboxylic ester derivatives. DR. A. WANDER Ltd. 16 Oct., 1969 [8 Nov., 1968; 28 Feb., 1969; 5 Aug., 1969], No. 50806/69. Heading C2C. Novel compounds I in which Z is O or S and R is alkyl, haloalkyl, alkoxyalkyl, alkenyl, cycloalkyl or cycloalkylalkyl and their acid addition salts are prepared (1) by reaction of a compound II where X is a reactive radial, with morpholine or thiamorpholine; (2) by reaction of a compound I in which R is H with ROH; (3) by reaction of halogen or hydrogen halide with a compound I in which R is alkenyl to give I in which R is haloalkyl; (4) splitting off vicinal halogen atoms, hydrogen halide or water from a compound I in which R is alkyl substituted by halo or hydroxy to give I in which R is alkenyl; or (5) hydrogenating a compound I where R is an unsaturated radical to obtain the corresponding saturated ester. Compounds I where R is 1-9C hydroxyalkyl are also novel but not said to be pharmaceutically active. Intermediates isolated are compounds II where X is halo and R is alkyl or H and compounds I where R is H. Pharmaceutical compositions comprise a compound I where R is alkyl, haloalkyl, alkoxyalkyl, alkenyl, cycloalkyl or cycloalkylalkyl and a suitable excipient. They have soporific and narcotic activity. |
