Pyrimidinyl aminomethylenemalonates analogs and intermediates

Details Pyrimidinyl aminomethylenemalonates analogs and intermediates Pyrimidinyl aminomethylenemalonates analogs and intermediates

C - Chemistry, Metallurgy

07

D

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C07D 401/04 (2006.01) A61K 31/505 (2006.01) C07D 213/04 (2006.01) C07D 239/28 (2006.01)

Patent

CA 1051431

ABSTRACT OF THE DISCLOSURE 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 Image is Image 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-(R5R6N)-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.

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