发明名称 |
PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF |
摘要 |
The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride 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-butoxycarbonyl)amino]-cyclohexyl}-acetic acid ester with sodium borohydride and aluminum 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 obtained 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. |
申请公布号 |
EP2358690(B1) |
申请公布日期 |
2016.03.30 |
申请号 |
EP20090797145 |
申请日期 |
2009.12.17 |
申请人 |
RICHTER GEDEON NYRT. |
发明人 |
CZIBULA, LÁSZL;ÁGAINÉ CSONGOR, ÉVA;NOGRADI, KATALIN;JUHASZ, BÁLINT;SEBOK, FERENC;GALAMBOS, JÁNOS;VAGO, ISTVÁN |
分类号 |
C07D295/135 |
主分类号 |
C07D295/135 |
代理机构 |
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代理人 |
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主权项 |
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