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    Alkenyl-substituted thienylalkanecarboxylic acids and derivatives thereof
    7.
    发明授权
    Alkenyl-substituted thienylalkanecarboxylic acids and derivatives thereof 失效
    烯基取代的噻吩烷基羧酸及其衍生物

    公开(公告)号：US4309407A

    公开(公告)日：1982-01-05

    申请号：US206077

    申请日：1980-11-12

    申请人： Hans-Heiner Lautenschlager ,  Hans Betzing ,  Johannes Winkelmann ,  Manfred Probst

    发明人： Hans-Heiner Lautenschlager ,  Hans Betzing ,  Johannes Winkelmann ,  Manfred Probst

    IPC分类号： A61K31/38 ,  A61K31/381 ,  A61P9/10 ,  A61P29/00 ,  C07D333/24

    CPC分类号： C07D333/24

    摘要： The invention provides novel .omega.-(5-alkenylthien-2-yl)alkanecarboxylic acids and their functional derivatives having the formula ##STR1## wherein n is an integer from 1 to 9, inclusive; R.sup.1 is H and R.sup.2 is --OH, or R.sup.1 and R.sup.2 together with the wavy lines represent a keto group; and R.sup.3 is H, C.sub.1 -C.sub.6 straight or branched-chain saturated hydrocarbon, or a pharmaceutically acceptable alkali cation. The 3-oxoalkenyl-substituted compounds of formula (I) are prepared by a Wittig-Horner reaction using a 2-oxoheptylphosphonic acid dialkyl ester and an aldehyde of the formula ##STR2## as starting materials, while the 3-hydroxyalkenyl-substituted compounds are obtained by reduction of the corresponding 3-oxoalkenyl compounds. The esters of formula (I) can also be readily converted to the corresponding acids and salts of formula (I).The compounds of the invention have valuable anti-inflammatory, antipyretic and anti-arteriosclerotic properties, yet have low toxicity and do not irritate the gastric mucosa.

    摘要翻译： 本发明提供新的ω-（5-烯基噻吩-2-基）烷羧酸及其具有式（I）的式（I）的功能性衍生物，其中n为1至9的整数，包括1和9的整数; R1是H，R2是-OH，R1和R2与波浪线一起代表酮基; 和R3是H，C1-C6直链或支链饱和烃或药学上可接受的碱性阳离子。 式（I）的3-氧代烯基取代的化合物通过使用2-氧代庚基膦酸二烷基酯和式“IMAGE”的醛作为起始原料的Wittig-Horner反应制备，而3-羟基烯基取代的化合物是 通过还原相应的3-氧代烯基化合物获得。 式（I）的酯也可以容易地转化为相应的式（I）的酸和盐。 本发明的化合物具有有价值的抗炎，解热和抗动脉硬化性质，但毒性低，不刺激胃粘膜。