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2. 发明申请

WO2011073705A1 NOVEL PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 审中-公开
标题翻译：制备哌嗪化合物及其盐酸盐的新工艺
公开(公告)号：WO2011073705A1
公开(公告)日：2011-06-23
申请号：PCT/HU2010/000144
申请日：2010-12-17
申请人： RICHTER GEDEON NYRT. , CZIBULA, Lászlό , JUHÁSZ, Bálint , ÁGAINÉ CSONGOR, Éva , SEBŐK, Ferenc , GALAMBOS, János , NÓGRÁDI, Katalin
发明人： CZIBULA, Lászlό , JUHÁSZ, Bálint , ÁGAINÉ CSONGOR, Éva , SEBŐK, Ferenc , GALAMBOS, János , NÓGRÁDI, Katalin
IPC分类号： C07D295/135
CPC分类号： C07D295/135
摘要： The invention relates to a new process for the preparation of compounds of general formula (I) wherein R 1 and R 2 represent independently hydrogen or C 1-6 alkyl with straight or branched chain optionally substituted with aryl group; or C 2-7 alkenyl containing 1-3 double bonds; or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifiuoro-C 1-6 alkoxy, C 1-6 -alkoxycarbonil, C 1-6 alkanoyl, aryl, C 1-6 alkylthio, halogen or cyano; or optionally substituted monocyclic, bicyclic or tricyclic C 3-14 cycloalkyl group; R 1 and R 2 together with the adjacent nitrogen form a saturated or unsaturated optionally substituted monocyclic or bicyclic heterocyclic ring which may contain further heteroatoms selected from oxygen, nitrogen, or sulphur atoms and hydrochloric acid salts and/or hydrates and/or solvates thereof, by dissolving or suspending trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence of a base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C 1-6 straight or branched chain, partially or fully halogenated C 1-2 alkyl or phenyl, Z is -O-R or -X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R 1 and R 2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.
摘要翻译：本发明涉及制备通式（I）化合物的新方法，其中R 1和R 2独立地表示氢或任选被芳基取代的直链或支链的C 1-6烷基; 或含有1-3个双键的C2-7烯基; 或任选被一个或多个C 1-6烷氧基，三氟-C 1-6烷氧基，C 1-6 - 烷氧羰基，C 1-6烷酰基，芳基，C 1-6烷硫基，卤素或氰基取代的单环，双环或三环芳基; 或任选取代的单环，双环或三环C 3-14环烷基; R1和R2与相邻的氮一起形成饱和或不饱和的任选取代的单环或双环杂环，其可以含有选自氧，氮或硫原子的其它杂原子和盐酸盐和/或其水合物和/或溶剂合物，通过溶解或将式（III）的反式4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺或其盐或其水合物或溶剂合物悬浮在惰性溶剂中碱的存在然后加入通式（VI）的碳酸衍生物，其中R是具有C 1-6直链或支链，部分或完全卤代的C 1-2烷基或苯基的烷基，Z是-OR或-X，其中 R是如上所述，X是卤素，并且其中R如上所述获得的通式（IV）化合物原位或任选地在分离状态下与通式（Ⅴ）的胺反应，其中R 1和R 2是如上所述，得到通式（I）的化合物），然后任选地形成盐酸盐和/或其水合物和/或溶剂合物。

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