合成路线1

The condensation of diethyl 2-(2-cyanoethyl)malonate (I) with 2-chloro-3-methyl-5-nitropyridine (II) by means of NaH in refluxing THF gives 4-(3-methyl-5-nitropyrid-2-yl)-4,4-bis(ethoxycarbonyl)butyronitrile (III), which is decarboxylated with NaOH in ethanol water yielding 4-(3-methyl-5-nitropyrid-2-yl)butyronitrile (IV). The reduction of (IV) with H2 over Pd/C in ethanol affords 4-(5-amino-3-methylpyrid-2-yl)butyronitrile (V), which is reduced further with LiAlH4 in ether-THF giving 5-amino-2-(4-aminobutyl)-3-methylpyridine (VI). The Sandmeyer reaction of (VI) with NaNO2, HBr and Cu2Br2 yields 5-bromo-2-(4-aminobutyl)-3-methylpyridine (VII), which is finally condensed with 2-nitroamino-5-(6-methylpyrid-2-ylmethyl)-4-pyrimidone (VIII) in refluxing pyridine.