Piperazine salt and a process for the preparation thereof

Details Piperazine salt and a process for the preparation thereof Piperazine salt and a process for the preparation thereof

C - Chemistry, Metallurgy

07

D

C07D 295/135 (2006.01)

Patent

CA 2743924

The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)- piperazine-1-il]-ethyl}- cyclohexylamine di- hydrochloride monohydrate and a process for the preparation of the trans N-{4- {2-[4-(2,3-dichlorophenyl)-piperazine-1-il]- ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{1-[4-(N-tert-butoxy- carbonyl)amino]- cyclohexyl} -acetic acid ester with sodium borohydride and aluminium trichloride to give trans 2-{1-[4-(N-tert- butoxycarbonyl)-amino]-cyclohexyl} -ethanol; b) reacting trans 2-{1-[4-(N-tert- butoxycarbonyl)-amino]cyclohexyl} -ethanol ob- tained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)- amino] -cyclohexyl} -ethyl methanesulfonate; c) reacting trans 2-{1-[4-(N-tert- butoxycarbonyl)-amino]-cyclohexyl} -ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{1-[4-(N- tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester; d) heating trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]- cyclohexyl}-carbamic acid tert- butylester obtained to a temperature between 40-100°C in a mixture of aqueous hydrochloric acid/ methanol to give trans N-{4-{2-[4-(2,3-dichlorophenyl)piperazine-1-il]-ethyl }- cyclohexylamine dihydrochloride monohydrate.

L'invention concerne un nouveau trans N-{4-{2-[4-(2,3-dichlorophényl)-pipérazine-l-il]-éthyl}- cyclohexylamine dihydrochlorure monohydrate et son procédé de préparation. Ledit procédé consiste: a) à faire réagir l'ester d'acide acétique trans 2-{l-[4-(N-tert-butoxycarbonyl)amino]- cyclohexyl} avec du borohydrure de sodium et le trichlorure d'aluminium pour obtenir trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-éthanol; b) à faire réagir trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-éthanol obtenu avec le chlorure d'acide méthanesulfonique en présence d'un agent de liaison acide pour obtenir trans 2-{l-[4- (N-tert-butoxycarbonyl)-amino] -cyclohexyl} -éthyl méthanesulfonate; c) à faire réagir trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-éthyl méthanesulfonate obtenu avec 2,3-dichlorophényl-pipérazine en présence d'un agent de liaison acide pour obtenir trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-acide carbamique tert-butylester obtenu vers une température comprise entre 40-100°C dans un mélange acide chlorhydrique/méthanol aqueux pour obtenir trans N-{4-{2-[4-(2,3-dichlorophényl)pipérazine-l-il]-éthyl}- cyclohexylamine dihydrochlorure monohydrate.

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