Preparation of chalcone derivatives
    1.
    发明授权
    Preparation of chalcone derivatives 有权
    查耳酮衍生物的制备

    公开(公告)号:US08765992B2

    公开(公告)日:2014-07-01

    申请号:US13698832

    申请日:2011-05-16

    摘要: The invention relates to methods for producing chalcone (1,3-diphenylprop-2-en-1-one) derivatives that have multiple substitutions on a phenyl ring. Intermediate chalcone derivatives are modified by Phase Transfer Catalysis (PTC) for introducing a substituted alkyl group that is provided by a sulfonic acid derivative on a phenyl ring already containing substituent groups on one or two carbon atoms adjacent to the carbon atom where a substituent group is being introduced. The methods of the invention allow producing efficiently, by either S-alkylation or O-alkylation, chalcones derivatives that are characterized for their biological activities that are intermediate compounds for producing molecules having such activities, or that can be used for generating libraries of compounds to be screened by means of in vitro and/or in vivo assays and establishing structure-activity relationships.

    摘要翻译: 本发明涉及在苯环上具有多个取代基的查尔酮(1,3-二苯基丙-2-烯-1-酮)衍生物的方法。 中间查耳酮衍生物通过相转移催化剂(PTC)进行改性,用于将由磺酸衍生物提供的取代的烷基引入到已经含有一个或两个邻近碳原子上的取代基的取代基的苯环上,其中取代基为 被介绍 本发明的方法允许通过S-烷基化或O-烷基化有效生产由其生物活性表征的作为用于产生具有这种活性的分子的中间体化合物的或可以用于产生化合物文库的查尔酮衍生物 通过体外和/或体内测定法筛选并建立结构 - 活性关系。

    PREPARATION OF CHALCONE DERIVATIVES
    2.
    发明申请
    PREPARATION OF CHALCONE DERIVATIVES 有权
    喹诺酮衍生物的制备

    公开(公告)号:US20130131372A1

    公开(公告)日:2013-05-23

    申请号:US13698832

    申请日:2011-05-16

    摘要: The invention relates to methods for producing chalcone (1,3-diphenylprop-2-en-1-one) derivatives that have multiple substitutions on a phenyl ring. Intermediate chalcone derivatives are modified by Phase Transfer Catalysis (PTC) for introducing a substituted alkyl group that is provided by a sulfonic acid derivative on a phenyl ring already containing substituent groups on one or two carbon atoms adjacent to the carbon atom where a substituent group is being introduced. The methods of the invention allow producing efficiently, by either S-alkylation or O-alkylation, chalcones derivatives that are characterized for their biological activities that are intermediate compounds for producing molecules having such activities, or that can be used for generating libraries of compounds to be screened by means of in vitro and/or in vivo assays and establishing structure-activity relationships.

    摘要翻译: 本发明涉及在苯环上具有多个取代基的查尔酮(1,3-二苯基丙-2-烯-1-酮)衍生物的方法。 中间查耳酮衍生物通过相转移催化剂(PTC)进行改性,用于将由磺酸衍生物提供的取代的烷基引入到已经含有一个或两个邻近碳原子上的取代基的取代基的苯环上,其中取代基为 被介绍 本发明的方法允许通过S-烷基化或O-烷基化有效生产由其生物活性表征的作为用于产生具有这种活性的分子的中间体化合物的或可以用于产生化合物文库的查尔酮衍生物 通过体外和/或体内测定法筛选并建立结构 - 活性关系。