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    Novel 5-Aminomethylene-2,4-imidazolidinediones and 5-aminomethylene-2-thionoimidazolidine-4-ones
    211.
    发明公开
    Novel 5-Aminomethylene-2,4-imidazolidinediones and 5-aminomethylene-2-thionoimidazolidine-4-ones 失效
    5-氨基亚甲基-2,4-咪唑烷二酮和5-氨基亚甲基-2-硫代咪唑烷-4-酮。

    公开(公告)号：EP0300882A2

    公开(公告)日：1989-01-25

    申请号：EP88401828.4

    申请日：1988-07-13

    申请人： ICI AMERICAS INC.

    发明人： Prisbylla, Michael Paul

    IPC分类号： C07D233/96 ,  C07D401/12 ,  C07D403/12 ,  A01N43/50

    CPC分类号： C07D401/06 ,  A01N43/50 ,  C07D233/96 ,  C07D401/12 ,  C07D403/06

    摘要： Compounds having the formula:
    wherein:

    R is alkyl, phenyl, substituted phenyl, alkylsulfonyl, alkoxy, halo,
    or haloalkyl;
    R 1 is hydrogen, alkyl, phenyl or halo substituted phenyl;
    R 2 is hydrogen or alkyl;
    R 3 is

    wherein:
    R 4 and R 5 are independently hydrogen, alkyl, phenyl, halophenyl, phenalkyl, halophenalkyl, cycloalkyl, cycloalkylmethyl, naphthyl, pyridyl, pyridylalkyl, or R 4 and R 5 taken together with nitrogen form hexamethyleneimine, piperidine, phenylpiperidine, benzylpiperidine, indoline, or perhydroindole; and
    V is oxygen or sulfur;
    provided that when R 1 is methyl and R 3 is

    wherein R 4 is methyl and R 5 is phenyl, then R is other than 2-chlorophenyl or 2-methoxyphenyl; and when R 1 is hydrogen or ethyl and R 3 is

    wherein R 4 is methyl and Rs is phenyl, then R is other than 3,4-dichlorophenyl;
    and herbicidal compositions and methods utilizing said compounds.

    摘要翻译： 具有下式的化合物：其中：R是烷基，苯基，取代的苯基，烷基磺酰基，烷氧基，卤素或卤代烷基; R1是氢，烷基，苯基或卤素取代的苯基; R2是氢或烷基; R3是其中：R4和R5独立地是氢，烷基，苯基，卤代苯基，苯基烷基，卤代烷基，环烷基，环烷基甲基，萘基，吡啶基，吡啶基烷基或R4和R5与氮一起形成六亚甲基亚胺，哌啶，苯基哌啶，苄基哌啶 ，二氢吲哚或全氢吲哚; V是氧或硫; 条件是当R 1是甲基且R 3是，其中R 4是甲基且R 5是苯基时，则R不是2-氯苯基或2-甲氧基苯基; 当R 1为氢或乙基且R 3为，其中R 4为甲基且R 5为苯基时，则R不为3,4-二氯苯基; 以及利用所述化合物的除草组合物和方法。

    Processes using a phosphorus complex
    215.
    发明公开
    Processes using a phosphorus complex 失效
    Verfahren unter Verwendung eines Phosphor-Komplexes。

    公开(公告)号：EP0283270A2

    公开(公告)日：1988-09-21

    申请号：EP88302305.3

    申请日：1988-03-16

    申请人： ICI AMERICAS INC.

    发明人： Timony, Peter Edward ,  Bay, Elliott ,  Leone-Bay, Andrea

    IPC分类号： C07F9/54 ,  C07B39/00

    CPC分类号： C07C17/093 ,  C07B39/00 ,  C07C17/16 ,  C07C22/06 ,  C07C19/01 ,  C07C25/06

    摘要： A process for the preparation of a phosphorus complex corresponding to the following general formula:
    wherein R represents optionally substituted aryl, wherein the substitution may comprise at least one selected from nitro, chloro, fluoro, alkyl, fluoro-alkyl and alkoxy, or optionally substituted alkyl; characterised in that it comprises reacting phosphorus pentachloride and a phosphonic dichloride corresponding to the following general formula:
        RPOCl₂
    wherein R is as defined above; in the presence of an inert solvent boiling at a temperature of from 120 to 150°C, which is capable of co-distilling a phosphorus oxychloride reaction product, and co-distilling a phosphorus oxychloride reaction product, the molar ratio of phosphorus pentachloride:phosphonic dichloride being from 0.1:1 to 10:1 is disclosed.
    There is further disclosed a process for chlorinating compounds containing a carbon atom bonded to a hetero-atom selected from oxygen, nitrogen and sulfur which comprises contacting the carbon hetero-atom containing compound with a chloro phosphorus complex corresponding to the following general formula:
    wherein R represents optionally substituted aryl or optionally substituted alkyl, so that the hetero-atom is replaced by at least one chlorine atom; the reaction may be extended to compounds containing the carbon to chlorine bond alpha to a carbon atom having at least one hydrogen atom, it may be further dehydrochlorinated by either heating to a temperature of from 50 to 300°C or by reaction with a selected base.

    摘要翻译： 一种制备对应于下列通式的磷络合物的方法：其中R代表任意取代的芳基，其中取代基可以包括选自硝基，氯，氟，烷基，氟 - 烷基和烷氧基中的至少一种， 或任选取代的烷基; 其特征在于它包括使五氯化磷与对应于以下通式的膦酰氯反应：RPOCl 2，其中R如上定义; 在沸点为120〜150℃的惰性溶剂的存在下，其能够共同蒸馏三氯氧化磷反应产物，并共同蒸馏出三氯氧化磷反应产物，五氯化磷：膦酸的摩尔比 公开了二氯化物为0.1:1至10:1。 还公开了一种氯化含有与选自氧，氮和硫的杂原子键合的碳原子的化合物的方法，该方法包括使含碳杂杂原子的化合物与对应于以下通式的氯磷络合物接触：其中R表示任选取代的芳基或任选取代的烷基，使得杂原子被至少一个氯原子代替; 该反应可以延伸至含有至少一个氢原子的碳原子的碳与氯键的化合物，也可以通过加热至50至300℃的温度或通过与选定的碱反应而进一步脱氯化氢 。

    Substituted peptide derivatives
    217.
    发明公开
    Substituted peptide derivatives 失效
    取代肽衍生物。

    公开(公告)号：EP0276101A2

    公开(公告)日：1988-07-27

    申请号：EP88300343.6

    申请日：1988-01-15

    申请人： ICI AMERICAS INC.

    发明人： Lewis, Joseph James ,  Perkins, Charles William ,  Trainor, Diane Amy ,  Wildonger, Richard Alan

    IPC分类号： C07K5/00 ,  A61K37/64

    CPC分类号： C07K5/06191 ,  A61K38/00

    摘要： The invention provides a series of novel substituted peptide derivatives of the formulae la, Ib and Ic (set out hereinafter) and pharmaceutically acceptable salts thereof, in which the radicals A, R 1 , R 2 and R 4 -R 9 have the meanings defined in the following specification. The compounds of formulae la, Ib, and Ic are inhbitors of human leukocytic elastase. The invention also provides pharmaceutical compositions containing a compound of formula la, Ib or Ic, or a pharmaceutically acceptable salt thereof and processes and intermediates for the manufacture of compounds of formulae la, Ib, and Ic.

    摘要翻译： 本发明提供了一系列新颖的式Ia，Ib和Ic的取代肽衍生物（下文阐述）及其药学上可接受的盐，其中基团A，R 1，R 2和R 2， 4> -R 9具有以下说明书中定义的含义。 式Ia，Ib和Ic的化合物是人白细胞弹性蛋白酶的抑制剂。 本发明还提供含有式Ia，Ib或Ic化合物或其药学上可接受的盐的药物组合物和用于制备式Ia，Ib和Ic化合物的方法和中间体。