Method for producing 4-(heteroaryl-methyl)-1(2h)-phthalazinones

Details Method for producing 4-(heteroaryl-methyl)-1(2h)-phthalazinones Method for producing 4-(heteroaryl-methyl)-1(2h)-phthalazinones

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) C07D 403/06 (2006.01)

Patent

CA 2395407

A process for the production of 4-(heteroaryl-methyl)-halogen-1(2H)-- phthalazinones, especially4-(4-pyridylmethyl)-1(2H)-phthalazinone, is described, which is characterized by the reaction of phthalidyl-3-triphenylphosphonium salt with 4-pyridine aldehyde in the presence of a basic adjuvant, subsequent reaction with hydrazine hydrate and subsequent acid treatment, whereby this process avoids the technical safety and environmental problems of the known processes.

L'invention concerne un procédé permettant de préparer des 4-(hétéroaryle-méthyle)-halogène-1(2H)-phtalazinones, notamment de la 4-(4-pyridylméthale)-1(2H)phtalazinone. Ce procédé se caractérise par la réaction de sel de phtalidyle-3-triphénylphosphonium avec du 4-pyridinaldéhyde en présence d'un auxiliaire basique, puis par la réaction avec de l'hydrate d'hydrazine et enfin par le traitement à l'acide. Ce procédé évite les problèmes techniques touchant la sécurité et l'environnement, inhérents aux procédés connus.

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