SYNTHESIS OF PLURIAMINATED PYRIDINES

The key reagent 3,5-dichloro-4-pyridinecarbonitrile (1) was used to sy nthesize 4-aminomethylpyridine derivatives 3,5-disubstituted with vari ous amino groups, very active as inhibitors of diamine oxidase. The st udy of the reaction allowed to discover conditions for the gradual sub stitution in good yields of the two chlorine atoms to give symmetrical ly and unsymmetrically disubstituted derivatives (3), or the substitut ion of the cyano group, or the formation of amidines. The reduction of the cyano to aminomethyl group in compounds (3) afforded the target b ioactive products.