| 摘要 |
Novel quaternary 5-ammonium-methyl-4-amino-2-R-pyrimidine salts, in which R represents a cycloaliphatic group and the ammonium nitrogen atom is part of a monocyclic or bicyclic heterocyclic radical containing one or more double bonds, one of which extends from the ammonium nitrogen atom, are prepared by reacting a reactive ester or ether of a 4-amino-5-hydroxymethyl - 2 - R - pyrimidine with a monocyclic or bicyclic heterocyclic compound containing at least one ring nitrogen atom and one or more double bonds, one of which extends from the ring nitrogen atom. 4 - Amino - 5 - hydroxymethyl - 2 - R - pyrimidines are prepared by reacting an R-halide with sodium cyanide to form the corresponding R-cyanide, reacting this an alkanol to form the corresponding alkyl R-carboximidate, reacting this with ammonia to form the corresponding R-carboxylic acid amidine, reacting this with a C1- 7 alkoxymethylene-malonitrile to form a 4-amino - 5 - cyano - 2 - R - pyrimidine, hydrogenating this to the corresponding 5-aminomethyl compound and converting this into the corresponding 5-hydroxymethyl compound by treatment with nitrous acid. Alternatively, the 5-cyano compound may be hydrogenated in the presence of hydrochloric acid to form the 5-hydroxymethyl compound directly. Cyclobutylmethyl bromide is prepared by treating cyclobutane carboxylic acid with lithium aluminium hydride to form cyclobutylmethanol and treating this with phosphorus tribromide. Cyclopropylmethyl bromide is similarly prepared via cyclopropylmethanol. 4 - Amino - 5 - chloromethyl - 2 - cyclopropylmethyl-pyrimidine hydrochloride is prepared by reacting 4-amino-5-hydroxymethyl-2-cyclopropylmethyl-pyrimidine with thionyl chloride. |
