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Paper | Regular issue | Vol 41, No. 4, 1995, pp.675-688
Published online, 1st January, 1970
DOI: 10.3987/COM-94-6945
3,5-Dichloro-4-pyridinecarbonitrile as a Key Reagent in a Synthesis of Copper Containing Amine Oxidase Inhibitors

Vincenzo Bertini, Francesco Lucchesini, Marco Pocci, and Angela De Munno

*Instituto di Analisi e Tecnologie Farmaceutiche ed Alimentari, Università di Genova, Via Brigata Salerno, I-16147 Genova, Italy

Abstract

Various synthetic approaches to 3,4,5-trifunctionalized pyridine derivatives useful as benzylamine oxidase inhibitors are extensively explored. Fully satisfactory preparations of the inhibitors 3,5-diethoxy-4-aminomethylpyridine (4), 3,5-bis(3-hydroxypropoxy)-4-aminomethylpyridine (11), 3,5-bis(4-hydroxybutoxy)-4-aminomethylpyridine (12) and 3-ethoxy-5-phenylmethoxy-4-aminomethylpyridine (16), all in the form of dihydrochloride salt, using 3,5-dichloro-4-pyridinecarbonitrile as key precursor, are reported.