| 摘要 |
<p>HYPNOTIC AND SEDATIVE 2,4-BIS-MORPHOLINO- AND THIAMORPHOLINO-5-CARBOXY PYRIMIDINE ESTERS. M3A. are new compounds of formula (I) including their addition salts. (Z = O or S; R = alkyl opt. substd. by 1-4 halogens. esp. F, Cl, Br, alkyl substd. by one or more OH groups, or alkenyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl (all is not > C9)). Used as narcotic and hypnotics in man and animals with a greater therapeutic index than of pentobarbitone. ED50 i.v. in mice of 4-22 mg/kg compared with 33 mg/kg for sodium pentobarbitone. 2,4-Bis-morpholino-5-isobutoxycarbonyl-pyrimidine has ED50/LD50 of 4/59 compared with 33/80 for Na pentobarbitone. Preferred dose 125-500 mg for adults. Prepared by various methods eg. (X = reactive group).</p> |
