4-Acylamino-2-(pyridinyl)pyrimidine derivatives

Details 4-Acylamino-2-(pyridinyl)pyrimidine derivatives 4-Acylamino-2-(pyridinyl)pyrimidine derivatives

1977-11-30

1978-10-03

Coughlan, Jr., Paul M.

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544328, C07D40104

Patent

active

041185714

ABSTRACT:
Compounds useful as anti-allergic agents are 2-Q-4-[XZC.dbd.C(R)NH]-5-R.sub.1 -6-R.sub.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.sub.1 is hydrogen, lower-alkyl or cyano, R.sub.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## is ##STR2## where R.sub.3 and R.sub.4 are each lower-alkyl, or X is hydrogen, are prepared by reacting 4-amino-2-Q-5-R.sub.1 -6-R.sub.2 -pyrimidine (II where Q' is amino) with R'O--C(R).dbd.CXZ (III). Preparations of II are given. Also shown as intermediates and/or anti-allergic agents are 4-(AcNH)-2-Q-5-R.sub.1 -6-R.sub.2 -pyrimidines (IV) and 4-(R.sub.5 R.sub.6 N)-2-Q-5-R.sub.1 -6-R.sub.2 -pyrimidines (V) where Ac is lower-alkanoyl or lower-carbalkoxy, R.sub.5 is hydrogen, lower-alkyl or lower-hydroxyalkyl, and R.sub.6 is lower-alkyl or lower-hydroxyalkyl.

REFERENCES:
lafferty et al., J. Org. Chem., 32(5), pp. 1591-1596 (1967).

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