4-Amino-6-arylpyrimidines and salts thereof, a novel class of inhibitors of platelet aggregation and broncho-dilators in mammals, and 4-hydroxy-6-arylpyrimidines as useful intermediates.
This application is a divisional of application Ser. No. 371,483 filed June 19, 1973, now U.S. Pat. No. 3,895,112, which is a divisional of application Ser. No. 182,220 filed Sept. 20, 1971 now U.S. Pat. 3,859,288 which is a continuation in part of application Ser. No. 78,216 filed Oct. 5, 1970 now abandoned.
A process for preparing a 4-hydroxypyrimidine of Formula III: ##STR1## wherein R.sub.1 and R.sub.2 each represent a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms or an aralkyl group having 2 to 10 carbon atoms, and R.sub.4 represents hydrogen an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms, an aralkyl group having 7 to 10 carbon atoms or an aryl group having 6 to 10 carbon atoms, which comprises subjecting a 3-amino-2-unsaturated carboxylate of Formula I: ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.3 represents an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms or an aralkyl group having 7 to 10 carbon atoms, and a carboxylic acid amide of Formula II: wherein R.sub.4 is as defined above, to reaction with each other in the presence of a base.
The invention relates to pyrimidine compounds of the formula: ##STR1## wherein the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as herein defined, having activity as a cardiotonic, anti-hypertensive, cerebrovascular vasodilator and anti-platelet aggregation agent.
Herein is disclosed amino-pyrimidine derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for increasing cardiac contractility in a mammal.
