61310-40-5Relevant academic research and scientific papers
N-[2-(pyridinyl)-4-pyrimidinyl]ureas
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, (2008/06/13)
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 or lower-hydroxyalkyl, R4 is hydrogen, lower-alkyl, lower-hydroxyalkyl, lower-alkenyl or lower-cycloalkyl. Said ureas are prepared by reacting 2-Q-4-RNH-5-R1 -6-R2 -pyrimidine (II) with a carbamylating agent selected from an R4 '-isocyanate of the formula R4 'N=C=O to produce N-R4 '-N'-R-N'-(2-Q-5-R1 -6-R2 -4-pyrimidinyl)urea (IA), an N-R3 '-N-R4 '-carbamyl halide of the formula R3 'R4 'NC(=O)-halide to produce N-R3 '-N-R4 '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 R3 R4 NH to produce I.
N-(2-(pyridinyl)-4-pyrimidinyl)-aminomethylenemalonates and analogs
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, (2008/06/13)
Compounds useful as anti-allergic agents are 2-Q-4-[XZC=C(R)NH]-5-R1 -6-R2 -pyrimidines (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, lower-alkyl, hydroxy or halo, X and Z are the same or different and are each selected from lower-carbalkoxy, lower-alkanoyl, carbamyl and cyano, or STR1 where R3 and R4 are each lower-alkyl, or X is hydrogen, are prepared by reacting 4-amino-2-Q-5-R1 -6-R2 -pyrimidine (II where Q' is amino) with R'O-C-(R)=CXZ (III). Preparations of II are given. Also shown as intermediates and/or anti-allergic agents are 4-(AcNH)-2-Q-5-R1 -6-R2 -pyrimidines (IV) and 4-(R5 R6 N)-2-Q-5-R1 -6-R2 -pyrimidines (V) where Ac is lower-alkanoyl or lower-carbalkoxy, R5 is hydrogen, lower-alkyl or lower-hydroxyalkyl, and R6 is lower-alkyl or lower-hydroxyalkyl.
