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    Method for making cyclopropene inclusion complex
    5.
    发明公开
    Method for making cyclopropene inclusion complex 有权
    Verfahren zur Herstellung von Cyclopropen-Einschlusskomplexen

    公开(公告)号：EP2057899A3

    公开(公告)日：2009-07-22

    申请号：EP08166736.2

    申请日：2008-10-16

    申请人： Rohm and Haas Company

    发明人： Jacobson, Richard Martin

    IPC分类号： A01N27/00

    CPC分类号： C07C13/04 ,  C07C2601/02 ,  C08B37/0015

    摘要： There is provided batch methods of making cyclopropene complex involving mixture comprising (i) one or more molecular encapsulating agent and (ii) solvent, wherein the ratio of the amount of said (i) to the amount of said (ii) is higher than the solubility of said molecular encapsulating agent in said solvent. There is also provided continuous methods of making cyclopropene complex in which the ratio of the rate of addition of molecular encapsulating agent to the rate of addition of solvent is higher than the solubility of said molecular encapsulating agent in said solvent.

    摘要翻译： 提供了制备涉及混合物的环丙烯络合物的分批方法，其包括（i）一种或多种分子包封剂和（ii）溶剂，其中所述（i）的量与所述（ii）的量的比例高于 所述分子包封剂在所述溶剂中的溶解度。 还提供连续的制备环丙烯络合物的方法，其中分子包封剂的加入速率与溶剂加入速率的比例高于所述分子包封剂在所述溶剂中的溶解度。

    A method to prepare cyclopropenes
    7.
    发明公开
    A method to prepare cyclopropenes 有权
    Verfahren zur Herstellung von Cyclopropenen

    公开(公告)号：EP1146028A1

    公开(公告)日：2001-10-17

    申请号：EP01302930.1

    申请日：2001-03-28

    申请人： ROHM AND HAAS COMPANY

    发明人： Jacobson, Richard Martin

    IPC分类号： C07B37/10 ,  C07C13/04 ,  C07C1/30 ,  C07C1/32

    CPC分类号： C07C1/30 ,  C07B37/10 ,  C07C1/322 ,  C07C13/04

    摘要： The present invention relates to a method to prepare cyclopropenes by combining an allyl compound of the formula:
    wherein:

    X is a leaving group; and
    R is hydrogen or a substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, phenyl or naphthyl group wherein the substituents are independently halogen, alkoxy, or substituted or unsubstituted phenoxy;
    with a non-nucleophilic strong base in an inert solvent in the presence of a catalytic amount of a non-nucleophilic, weaker base.

    摘要翻译： 本发明涉及通过将下式的烯丙基化合物：其中：X是离去基团的烯丙基化合物来制备环丙烯的方法; R是氢或取代或未取代的烷基，烯基，炔基，环烷基，环烷基烷基，苯基或萘基，其中取代基独立地为卤素，烷氧基或取代或未取代的苯氧基; 与非亲核强碱在惰性溶剂中，在催化量的非亲核的较弱碱的存在下。

    A PROCESS FOR THE PREPARATION OF CYCLOPROPYLACETYLENE
    9.
    发明公开
    A PROCESS FOR THE PREPARATION OF CYCLOPROPYLACETYLENE 失效
    VERFAHREN ZUR HERSTELLUNG VON CYCLOPROPYLACETYLEN

    公开(公告)号：EP1000001A1

    公开(公告)日：2000-05-17

    申请号：EP98938110.8

    申请日：1998-07-29

    申请人： Dupont Pharmaceuticals Company

    发明人： FORTUNAK, Joseph, M. ,  WANG, Zhe ,  YIN, Jianguo

    IPC分类号： C07C13/04 ,  C07C22/00

    CPC分类号： C07C51/353 ,  C07C1/30 ,  C07C13/04 ,  C07C17/093 ,  C07C51/38 ,  C07C2601/02 ,  C07C2601/04 ,  C07C22/00 ,  C07C57/26

    摘要： The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, cyclopropane carboxaldehyde is condensed with malonic acid to form 3-cyclopropylacrylic acid; 3-cyclopropylacrylic acid is halogenated to form (E,Z)-1-halo-2-cyclopropylethylene; and (E,Z)-1-halo-2-cyclopropylethylene is dehydrohalogenated to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.

    摘要翻译： 本发明一般涉及合成环己基乙炔的新方法，它是不对称合成（S）-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1 苯并恶嗪-2-酮; 一种有用的人类免疫缺陷病毒（HIV）逆转录酶抑制剂。 在此过程中，环丙烷甲醛与丙二酸缩合形成3-环丙基丙烯酸; 将3-环丙基丙烯酸卤化形成（E，Z）-1-卤代-2-环丙基乙烯; 和（E，Z）-1-卤代-2-环丙基乙烯脱卤化氢形成环丙基乙炔。 这种改进提供了廉价的，容易获得的起始材料到环丙基乙炔的高转化率，高的总产率，并且可以在工业规模上进行。