摘要 |
<p>Compounds useful as anti-allergic agents are N-R3-N-R4- N'-R-N'-(2-Q-5-R1-6-R2-4-pyrimidinyl)ureas (I), where Q is 4- or 3- or 2-pyridinyl or 4- or 3- or 2-pyridinyl having one or two lower-alkyl substituents or N-oxide thereof, R is hydrogen or lower-alkyl, R1 is hydrogen, lower-alkyl or cyano, R2 is hydrogen or lower-alkyl, R3 is hydrogen, lower-alkyl, lower-hydroxyalkyl or lower-dihydroxyalkyl, R4 is hydrogen, lower-alkyl, lower-hydroxy-alkyl, lower-alkenyl or lower-cycloalkyl. Said ureas are prepared by reacting 2-Q-4-RNH-5-R1-6-R2-pyrimidine (II) with an R?-iso-cyanate of the formula R?N=C=O to produce N-R?-N'-R-N'-(2-Q-5-R1-6-R2-4-pyrimidinyl)urea (IA), an N-R?-N-R?-carbamyl halide of the formula R?R?NC(=O)-halide to produce N-R?-N-R?-N'-R-N'-(2-Q-5-R1-6-R2-4-pyrimidinyl)urea (IB) or 1,1'-carbonyldiimidazole to produce N-(2-Q-5-R1-6-R2-4-pyrimidinyl)-N-R-imidazole-1-carboxamide and then reacting said 1-carboxamide with R3R4NH to produce I.</p> |