N-(2-(pyridinyl)-4-pyrimidinyl)-aminomethylenemalonates and analogs

Abstract

Abstract Compounds useful as anti-allergic agents are 2-Q-4-[XZC=C(R)NH]-5-R 1 -6-R 2 -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, R 1 is hydrogen, lower-alkyl or cyano, R 2 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 R 3 and R 4 are each lower-alkyl, or X is hydrogen, are prepared by reacting 4-amino-2-Q-5-R 1 -6-R 2 -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-R 1 -6-R 2 -pyrimidines (IV) and 4-(R 5 R 6 N)-2-Q-5-R 1 -6-R 2 -pyrimidines (V) where Ac is lower-alkanoyl or lower-carbalkoxy, R 5 is hydrogen, lower-alkyl or lower-hydroxyalkyl, and R 6 is lower-alkyl or lower-hydroxyalkyl.

Inventors

• 👤 George Y. Lesher
• 👤 Baldev Singh

Bibliographic Details