N-[2-(pyridinyl)-4-pyrimidinyl]ureas

Abstract

Abstract Compounds useful as anti-allergic agents are N-R 3 -N-R 4 -N'-R-N'-(2-Q-5-R 1 -6-R 2 -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, R 1 is hydrogen, lower-alkyl or cyano, R 2 is hydrogen or lower-alkyl, R 3 is hydrogen, lower-alkyl or lower-hydroxyalkyl, R 4 is hydrogen, lower-alkyl, lower-hydroxyalkyl, lower-alkenyl or lower-cycloalkyl. Said ureas are prepared by reacting 2-Q-4-RNH-5-R 1 -6-R 2 -pyrimidine (II) with a carbamylating agent selected from an R 4 '-isocyanate of the formula R 4 'N=C=O to produce N-R 4 '-N'-R-N'-(2-Q-5-R 1 -6-R 2 -4-pyrimidinyl)urea (IA), an N-R 3 '-N-R 4 '-carbamyl halide of the formula R 3 'R 4 'NC(=O)-halide to produce N-R 3 '-N-R 4 'N'-R-N'-(2-Q-5-R 1 -6-R 2 -4-pyrimidinyl)urea (IB) or 1,1'-carbonyldiimidazole to produce N-(2-Q-5-R 1 -6-R 2 -4-pyrimidinyl)-N-R-imidazole-1-carboxamide and then reacting said 1-carboxamide with R 3 R 4 NH to produce I.

Inventors

• 👤 George Y. Lesher
• 👤 Baldev Singh

Bibliographic Details