Biologically active tropane derivatives

Details Biologically active tropane derivatives Biologically active tropane derivatives

C - Chemistry, Metallurgy

07

D

C07D 451/02 (2006.01) A61K 31/435 (2006.01) A61K 31/46 (2006.01)

Patent

CA 2131789

Preparation of the biologically active tropane derivatives of formula (I) and structural isomers thereof wherein R equals C1 to C8 alkyl and Ar is an aromatic ring moiety. The compounds are prepared by decomposing vinyl-diazomethanes in the presence of pyrroles to provide a bicyclic ring containing the basic tropane ring system which is then reacted with an aryl Grignard reagent in the presence of a copper (I) or (II) salt to provide 3-aryl-tropane derivatives.

Préparation de dérivés du tropane biologiquement actifs, de formule (I) et de leurs isomères structuraux. Dans la formule, R est un alkyle contenant de 1 à 8 atomes de carbone, et Ar est un groupement cyclique aromatique. Les composés sont préparés par la décomposition de vinyldiazométhanes en présence de pyrroles, afin de produire un double cycle contenant le système cyclique de base du tropane, qui réagit ensuite avec un réactif de Grignard arylé en présence d'un sel de cuivre (I) ou (II) pour former des dérivés du 3-aryltropane.

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