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    • 4. 发明授权
    • Substituted [2-(1-piperazinyl)ethoxy]methyl compounds
    • 取代的[2-(1-哌嗪基)乙氧基]甲基化合物
    • US6140501A
    • 2000-10-31
    • US155977
    • 1998-10-09
    • Guy DucheneMichel DeleersGuy BodsonGenevieve MotteFrancoise Lurquin
    • Guy DucheneMichel DeleersGuy BodsonGenevieve MotteFrancoise Lurquin
    • C07D295/14C07D295/08C07D295/088C07D295/16C07D295/20C07D295/205C07D295/104C07D295/185
    • C07D295/088C07D295/205
    • Novel substituted [2-(1-piperazinyl)ethoxy]methyl compounds.The present invention related to novel substituted [2-(1-piperazinyl)-ethoxy]methyl compounds of formula ##STR1## in which R.sub.1 represents a --CONH.sub.2, --CN, --COOH, --COOM or --COOR.sub.3 group, M being an alkali metal and R.sub.3 being an alkyl radical having from 1 to 4 carbon atoms; andR.sub.2 represents a hydrogen atom or a group --COR.sub.4 or --R.sub.5, where R.sub.4 is chosen from the groups --OR.sub.6 or --R.sub.7, in whichR.sub.5 represents an allyl or alkylaryl radical,R.sub.6 represents a linear or branched alkyl radical having from 1 to 4 carbon atoms, a haloalkyl, alkylaryl, alkylnitroaryl or alkylhaloaryl radical, andR.sub.7 represents a haloalkyl radical,to a process for the preparation of these compounds, and to their use for the preparation of compounds which are themselves valuable intermediates for the preparation of 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid or 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]-acetic acid and/or pharmaceutically acceptable salts thereof.
    • PCT No.PCT / BE97 / 00038 Sec。 371日期:1998年10月9日 102(e)日期1998年10月9日PCT 1997年3月28日PCT公布。 第WO97 / 37982号公报 日期1997年10月16日新的取代的[2-(1-哌嗪基)乙氧基]甲基化合物。 本发明涉及其中R1表示-CONH2,-CN,-COOH,-COOM或-COOR3基团的新型取代的[2-(1-哌嗪基) - 乙氧基]甲基化合物,M为碱金属,R3为 是具有1至4个碳原子的烷基; 并且R 2表示氢原子或-COR 4或-R 5基团,其中R 4选自-OR 6或-R 7,其中R 5表示烯丙基或烷基芳基,R 6表示直链或支链烷基,其具有1至 4个碳原子,卤代烷基,烷基芳基,烷基硝基芳基或烷基卤代芳基,R7代表卤代烷基,用于制备这些化合物的方法,以及它们用于制备本身是制备2的有价值的中间体的化合物的用途 - [2- [4 - [(4-氯苯基)苯基甲基] -1-哌嗪基]乙氧基] - 乙酸或2- [2- [4- [二(4-氟苯基)甲基] -1-哌嗪基]乙氧基] - 乙酸和/或其药学上可接受的盐。
    • 6. 发明授权
    • Process of preparing [2-(1-piperazinyl)ethoxy]methyl compounds
    • 制备[2-(1-哌嗪基)乙氧基]甲基化合物的方法
    • US06255487B1
    • 2001-07-03
    • US09532159
    • 2000-03-21
    • Guy DucheneMichel DeleersGuy BodsonGenevieve MotteFrancoise Lurquin
    • Guy DucheneMichel DeleersGuy BodsonGenevieve MotteFrancoise Lurquin
    • C07D29510
    • C07D295/088C07D295/205
    • The present invention relates to novel substituted [2-(1-piperazinyl)-ethoxy]methyl compounds of formula in which R1 represents a —CONH2, —CN, —COOH, —COOM or —COOR3 group, M being an alkali metal and R3 being an alkyl radical having from 1 to 4 carbon atoms; and R2 represents a hydrogen atom or a group —COR4 or —R5, where R4 is chosen from the groups —OR6 l or —R7, in which R5 represents an alkyl or alkylaryl radical, R6 represents a linear or branched alkyl radical having from 1 to 4 carbon atoms, a haloalkyl, alkylaryl, alkylnitroaryl or alkylhaloaryl radical, and R7 represents a haloalkyl radical, to a process for the preparation of these compounds, and to their use for the preparation of compounds which are themselves valuable intermediates for the preparation of 2-[2-[4[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid or 2-[2-[4-[bix(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]-acetic acid and/or pharmaceutically acceptable salts thereof.
    • 本发明涉及R1代表-CON​​H 2,-CN,-COOH,-COOM或-COOR 3基团的新型取代的[2-(1-哌嗪基) - 乙氧基]甲基化合物,M是碱金属,R 3是 具有1至4个碳原子的烷基; 并且R 2表示氢原子或-COR 4或-R 5基团,其中R 4选自-OR 61或-R 7,其中R 5表示烷基或烷基芳基,R 6表示具有1-4个碳原子的直链或支链烷基 碳原子,卤代烷基,烷基芳基,烷基硝基芳基或烷基卤代芳基,R 7表示卤代烷基,制备这些化合物的方法,以及它们用于制备本身是制备2- [ 2- [4 [(4-氯苯基)苯基甲基] -1-哌嗪基]乙氧基] - 乙酸或2- [2- [4- [双(4-氟苯基)甲基] -1-哌嗪基]乙氧基] - 乙酸 和/或其药学上可接受的盐。