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    Novel intermediates for the synthesis of cephalosporins
    2.
    发明授权
    Novel intermediates for the synthesis of cephalosporins 失效
    用于合成头孢菌素的新型中间体

    公开(公告)号：US4782162A

    公开(公告)日：1988-11-01

    申请号：US872304

    申请日：1986-06-09

    申请人： Michael Boberg ,  Paul Naab ,  Samir Samaan

    发明人： Michael Boberg ,  Paul Naab ,  Samir Samaan

    IPC分类号： C07D277/20 ,  C07D277/44 ,  C07D277/46 ,  C07D501/20

    CPC分类号： C07D277/20

    摘要： The new compounds of the formula ##STR1## in which Acyl is alkylcarbonyl optionally substituted by halogen or aryl, or arylcarbonyl, which is substituted by lower alkoxy, halogen or nitro,R.sup.1 is an alkyl or alkenyl radical, andR.sup.4 is an optionally substituted branched or straight-chain C.sub.1 -C.sub.6 -alkyl radical or a cycloalkyl radical,are produced by reacting a 2-halogenoacetylacrylic acid ester of the formula ##STR2## with an acylthiourea of the formula ##STR3## The reaction can be conducted in aqueous DMF, substantially pure Z-isomer selectively crystallizing out.

    摘要翻译： 酰基为任选被卤素或芳基取代的烷基羰基或被低级烷氧基，卤素或硝基取代的芳基羰基的新化合物“IMAGE”，R1为烷基或烯基，R4为任选取代的支链 或直链C 1 -C 6 - 烷基或环烷基是通过使下式得到的式I的2-卤代乙酰基丙烯酸酯与下式的酰基硫脲反应制备的。反应可以在DMF水溶液中进行，基本上 纯Z-异构体选择性结晶出来。

    Process for the preparation of alkenyl esters of acemetacin
    3.
    发明授权
    Process for the preparation of alkenyl esters of acemetacin 失效
    乙酰丙酸烯基酯的制备方法

    公开(公告)号：US4658039A

    公开(公告)日：1987-04-14

    申请号：US800493

    申请日：1985-11-21

    申请人： Samir Samaan

    发明人： Samir Samaan

    IPC分类号： A61K31/405 ,  A61P29/00 ,  C07D209/28

    CPC分类号： C07D209/28

    摘要： The new indole derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and denote hydrogen or lower alkyl,R.sup.3 denotes hydrogen, lower alkyl or halogen andR.sup.4 and R.sup.5 are identical or different and denote hydrogen, lower alkyl or optionally substituted aryl, and R.sup.4 and R.sup.5 can also represent lower alkenyl, andwhereinR.sup.2 and R.sup.5 can be linked by an alkylene bridge of the formula--CH.sub.2 --CH.sub.2 --CH.sub.2).sub.nin whichn represents the number 0 or 1, can be prepared by reacting an ammonium or phosphonium salt of the corresponding indolecarboxylic acid with a haloacetic acid allyl ester. The new compounds can be used to prepare acemetacin. The new indole derivatives possess a pharmacological action.

    摘要翻译： 式中，R1和R2相同或不同，表示氢或低级烷基的新的吲哚衍生物，R3表示氢，低级烷基或卤素，R4和R5相同或不同，表示氢，低级烷基或任选地 取代的芳基，并且R 4和R 5也可以表示低级烯基，并且其中R 2和R 5可以被式-CH 2 -CH 2 -CH 2）n的亚烷基桥连接，其中n代表数字0或1，可以由 使相应的吲哚羧酸的铵盐或鏻盐与卤代乙酸烯丙基酯反应。 新化合物可用于制备acemetacin。 新的吲哚衍生物具有药理作用。