A process for the preparation of 1,4,7,10-tetraazacyclododecane

Details A process for the preparation of 1,4,7,10-tetraazacyclododecane A process for the preparation of 1,4,7,10-tetraazacyclododecane

C - Chemistry, Metallurgy

07

D

C07D 257/02 (2006.01)

Patent

CA 2288148

A process for the preparation of 1,4,7,10-tetraazacyclododecane of formula (I), starting from decahydro-2a,4a,6a,8a-tetraazacyclopent[fg]acenaphthylene of formula (II), comprising the direct step of hydrolysis in aqueous solution, in conditions of slightly acid, neutral or slightly basic pH, with a primary diamine of formula (V), in which x ranges between 0 and 2, and Q is -CH2CH(OH)CH2-, -(CH2)2NH(CH2)2-, or -[(CH2)2NH]2(CH2)2, when x is 1, or Q is -CH2- when x is 2.

L'invention concerne un procédé de préparation de 1,4,7,10-tétra-azacyclododécane de la formule (I), sur la base de décahydro-2a,4a,6a,8a-tétra-azacylopent[fg]acénaphtylène de la formule (II). Ce procédé comprend une étape directe d'hydrolyse en solution aqueuse, dans des conditions de pH légèrement acide, neutre ou légèrement basique, avec une diamine primaire de la formule (V), dans laquelle x est compris entre 0 et 2, et Q désigne -CH2CH(OH)CH2-, -(CH2)2NH(CH2)2-, ou -[(CH2)2NH]2(CH2)2, si x vaut 1, ou Q désigne -CH2- si x vaut 2.

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