(4)-Phenylamino-(2)-phenyl-pyrimidines with morpholino substituents - for protection against anoxia and are less toxic than vincamine

摘要

Pyrimidine derivs. of formula (I) and their intermediates (I:R is p-CO2Et) (where R1 is CH3 in which case R is COM, and Ar is phenyl opt. substd. by one halo or by 3 1-3C alkoxy at 3,4 and 5 posns.; or R1 is H, in which case R is O p-COM and Ar is o-halophenyl; or R is o- or m-COM and Ar is p-halophenyl; M is morpholino) are new. (I) protect against anoxia with an effectiveness comparable to vincamine but cause no deaths in mice when given orally at 1g/kg (c.f. 50% for vincamine). they are administered e.g. as 50-500 mg capsules 2-6 times/day or parenterally as 50-500 mg ampoules 1-3 times/day. In an example, reaction of (I: R is -p-CO2Et) with 2-morpholinoethylamine gave 4-(p-(2-morpholinoethyl)amino -carbonylanilino)-6-methyl-2-phenylpyrimidine.