A process for the preparation of tetraazamacrocycles

Details A process for the preparation of tetraazamacrocycles A process for the preparation of tetraazamacrocycles

C - Chemistry, Metallurgy

07

D

C07D 257/02 (2006.01) C07D 487/22 (2006.01)

Patent

CA 2258768

A process for the preparation of tetraazamacrocycles of general formula (I), wherein n, p and q can independently be 0 or 1, comprising the following steps: a) condensation of polyamines with a glyoxal derivative; b) condensation of the resulting compound with an alkylating agent; c) oxidation of the resulting compound with an oxidizing agent, to give a mixture of oxidated products which is submitted to d) hydrolysis in acid aqueous solution, to give the compound of formula (I).

L'invention concerne un procédé pour la préparation de tétraazamacrocycles selon la formule générale (I). Dans la formule, n, p et q peuvent indépendamment l'un de l'autre être égaux à O ou 1. Ce procédé comprend les étapes consistant à: a) condenser les polyamines avec un dérivé de glyoxal; b) condenser le composé obtenu avec un agent alkylant; c) oxyder le composé obtenu avec un agent oxydant pour donner un mélange de produits oxydés qui est soumis à d) une hydrolyse en solution aqueuse acide pour obtenir le composé selon la formule (I).

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