Process for the stereoselective preparation of (−)-halofenate and derivatives thereof
    27.
    发明授权
    Process for the stereoselective preparation of (−)-halofenate and derivatives thereof 失效
    ( - ) - 卤代苯甲酸酯及其衍生物的立体选择性制备方法

    公开(公告)号:US07714131B2

    公开(公告)日:2010-05-11

    申请号:US11525200

    申请日:2006-09-20

    IPC分类号: C07D295/16 C07D207/06

    CPC分类号: C07D295/185

    摘要: The present invention provides a compounds the formula (IV): and methods for producing an α-(phenoxy)phenylacetic acid compound of the formula: wherein R1 is a member selected from the group consisting of: each R2 is a member independently selected from the group consisting of (C1-C4)alkyl, halo, (C1-C4)haloalkyl, amino, (C1-C4)aminoalkyl, amido, (C1-C4)amidoalkyl, (C1-C4)sulfonylalkyl, (C1-C4)sulfamylalkyl, (C1-C4)alkoxy, (C1-C4)heteroalkyl, carboxy and nitro; the subscript n is 1 when R1 has the formula (a) or (b) and 2 when R1 has the formula (c) or (d); the subscript m is an integer of from 0 to 3; * indicates a carbon which is enriched in one stereoisomeric configuration; and the wavy line indicates the point of attachment of R1; and compounds.

    摘要翻译: 本发明提供式(Ⅳ)化合物及其制备下式所示的α-(苯氧基)苯乙酸化合物的方法:其中R 1为选自以下的成员:每个R 2为独立地选自 由(C 1 -C 4)烷基,卤素,(C 1 -C 4)卤代烷基,氨基,(C 1 -C 4)氨基烷基,酰胺基,(C 1 -C 4)酰氨基烷基,(C 1 -C 4)磺酰基烷基,(C 1 -C 4) ,(C 1 -C 4)烷氧基,(C 1 -C 4)杂烷基,羧基和硝基; 当R1具有式(a)或(b)时,下标n为1,当R1具有式(c)或(d))时,下标n为1; 下标m为0〜3的整数; *表示富含一种立体异构构型的碳; 波浪线表示R1的连接点; 和化合物。

    Substituted [2-(1-piperazinyl)ethoxy]methyl compounds
    29.
    发明授权
    Substituted [2-(1-piperazinyl)ethoxy]methyl compounds 有权
    取代的[2-(1-哌嗪基)乙氧基]甲基化合物

    公开(公告)号:US6140501A

    公开(公告)日:2000-10-31

    申请号:US155977

    申请日:1998-10-09

    CPC分类号: C07D295/088 C07D295/205

    摘要: 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.

    摘要翻译: 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。