A process for preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are lower alkoxy or taken together are METHYLENEDIOXY; R.sub.3 is lower alkyl or hydrogen, which comprises the step of reacting an aromatic compound of the formula ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are as previously described, with a diamino-pyrimidine of the formula ##STR3## wherein R.sub.4 is lower alkoxy, benzyloxy, hydroxy or halogen, in the presence of an inorganic or organic acid selected from the group consisting of ortho-phosphoric acid, poly-phosphoric acid, hydrohalic acids and tri-haloacetic acids, at a temperature in the range of from about 50.degree. C. to about 110.degree. C., is described.
CROSS REFERENCE TO RELATED APPLICATIONS
This is a continuation of application Ser. No. 564,518 filed Apr. 2, 1975, now abandoned, which in turn is a continuation of U.S. Patent Application Ser. No. 336,094 filed Feb. 26, 1973, now abandoned.
Novel substituted 2,4-diamino-5-benzyl pyrimidines are described. The novel substances have antimicrobial activity and are particularly suitable for inhibiting the growth of mycobacteria. Combined with inhibitors such as diaminodiphenylsulphones, ring-substituted 4-aminodiphenylsulphones or ring and/or nitrogen-substituted diaminodiphenylsulphones, they have a marked synergistic activity.
A process for preparing Tetroxoprim starting from 3,5-dimethoxy-4-methoxyethoxy-benzaldehyde and 2,4-diamino-6-hydroxy-pyrimidine, by successive hydrogenation, halogenation and hydrogenolysis of the 2,4-diamino-6-oxo-5-(3,5-dimethoxy-4-methoxyethoxy-benzylidene)-pyrimidine obtained in the initial reaction.
Compounds and methods for treating diseases mediated by a P2X.sub.3 and/or a P2X.sub.2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): ##STR00001## wherein D, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are as defined herein.
