| 摘要 |
<p>Pyrimidine derivs. of formula (I) are made by (a) reacting an amine of formula (II) with the acid chloride of formula (III) in an inert solvent, e.g. dioxane, toluene, MIBK or tetrahydrofurane, in presence of an acid acceptor, e.g. triethylamine, sodium or potassium carbonate, at 5-20 deg. C to give the intermediates of formula (IV); and (b) heating in the same medium to between 60 deg. C and b.pt. to form (I), which is isolated by the pption. with water, extraction wit solvent, e.q. methyl chloride, distn. to dryness and opt. salt formation with hydrochloric acid.</p> |
