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US 4,227,000 AGranted
Intermediates in the process for making histamine antagonists
AssigneeSmith Kline & French Laboratories Limited
InventorThomas H. Brown
Life of this patent
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Abstract
A process for making substituted 2-aminopyrimidones which are histamine H.sub.2 - antagonists which comprises reacting a 2-nitroaminopyrimidone with a heteroarylalkylamine, heteroarylalkylthioalkylamine, or heteroarylalkoxyalkylamine. One particular compound which can be made by this process is 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-[5-(1,3-benzodioxolyl) methyl]-4-pyrimidone. Also claimed are 2-nitroaminopyrimidone intermediates for use in this process. One specific intermediate is 2-nitroamino-5-[5-(1,3-benzodioxolyl)methyl]-4-pyrimidone.
Claims9
A 2-nitroaminopyrimidone of the formula:
- ##STR5## in which Z is hydrogen or lower alkyl, A is C.sub.1 -C.sub.5 alkylene or --(CH.sub.2).sub.p W(CH.sub.2).sub.q -- where W is oxygen or sulphur and the sum of p and q is 1 to 4, and B is a naphthyl, 5- or 6- (2,3-dihydro-1,4-benzodioxinyl), or 4- or 5- (1,3-benzodioxolyl) group, or a phenyl group substituted with lower alkyl, lower alkoxy, halogen, benzyloxy, hydroxy, lower alkoxy-lower alkoxy, trifluoromethyl, di(lower alkyl)amino, phenoxy, halophenoxy, lower alkoxy-phenoxy, phenyl, halophenyl or lower alkoxyphenyl groups.
Dependencies are inferred from the claim text.