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    Process for the preparation of dihydropyrrole derivatives
    6.
    发明授权
    Process for the preparation of dihydropyrrole derivatives 有权
    二氢吡咯衍生物的制备方法

    公开(公告)号：US09233920B2

    公开(公告)日：2016-01-12

    申请号：US13703630

    申请日：2011-06-14

    申请人： Myriem El Qacemi ,  Helmars Smits ,  Jerome Yves Cassayre ,  Nicholas Phillip Mulholland ,  Peter Renold ,  Edouard Godineau ,  Thomas Pitterna

    发明人： Myriem El Qacemi ,  Helmars Smits ,  Jerome Yves Cassayre ,  Nicholas Phillip Mulholland ,  Peter Renold ,  Edouard Godineau ,  Thomas Pitterna

    IPC分类号： C07D207/46 ,  C07D207/20 ,  C07D401/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  A01N43/36

    CPC分类号： C07D207/46 ,  A01N43/36 ,  C07D207/20 ,  C07D401/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R1 and R2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R1 and R2 are as defined for the compound of formula I; and (a-ii) reductively cyclizing the compound of formula III to give the compound of formula I. The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).

    摘要翻译： 本发明提供了制备式（I）化合物的立体选择性方法，其中P是苯基，萘基，含有一个或两个氮原子作为环成员的6元杂芳基或含有一个或多个氮原子的10元双环杂芳基 两个氮原子作为环成员，并且其中苯基，萘基和杂芳基任选被取代; R1是氯二氟甲基或三氟甲基; R2是任选取代的芳基或任选取代的杂芳基; n为0或1; 包括（a-i）使式II化合物与式Ⅰ化合物反应的方法，其中P，R 1和R 2如对式I化合物所定义; 在硝基甲烷中存在手性催化剂，得到式III化合物，其中P，R 1和R 2如式I化合物所定义; 和（a-ii）将式III化合物还原性环化得到式I化合物。本发明还提供了可用于合成式（I）化合物的方法的中间体。

    PROCESS FOR THE PREPARATION OF DIHYDROPYRROLE DERIVATIVES
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF DIHYDROPYRROLE DERIVATIVES 有权
    制备二氢衍生物衍生物的方法

    公开(公告)号：US20130237583A1

    公开(公告)日：2013-09-12

    申请号：US13703630

    申请日：2011-06-14

    申请人： Myriem El Qacemi ,  Helmars Smits ,  Jerome Yves Cassayre ,  Nicholas Phillip Mulholland ,  Peter Renold ,  Edouard Godineau ,  Thomas Pitterna

    发明人： Myriem El Qacemi ,  Helmars Smits ,  Jerome Yves Cassayre ,  Nicholas Phillip Mulholland ,  Peter Renold ,  Edouard Godineau ,  Thomas Pitterna

    IPC分类号： C07D207/46 ,  C07D207/20

    CPC分类号： C07D207/46 ,  A01N43/36 ,  C07D207/20 ,  C07D401/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R1 and R2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R1 and R2 are as defined for the compound of formula I; and (a-ii) reductively cyclising the compound of formula III to give the compound of formula I. The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).

    摘要翻译： 本发明提供了制备式（I）化合物的立体选择性方法，其中P是苯基，萘基，含有一个或两个氮原子作为环成员的6元杂芳基或含有一个或多个氮原子的10元双环杂芳基 两个氮原子作为环成员，并且其中苯基，萘基和杂芳基任选被取代; R1是氯二氟甲基或三氟甲基; R2是任选取代的芳基或任选取代的杂芳基; n为0或1; 包括（a-i）使式II化合物与式Ⅰ化合物反应的方法，其中P，R 1和R 2如对式I化合物所定义; 在硝基甲烷中存在手性催化剂，得到式III化合物，其中P，R 1和R 2如式I化合物所定义; 和（a-ii）还原性环化式III化合物以得到式I化合物。本发明还提供了可用于合成式（I）化合物的方法的中间体。