ESTERIFIED ANHYDROPENTITOLS AND METHODS OF MAKING THE SAME
    7.
    发明申请
    ESTERIFIED ANHYDROPENTITOLS AND METHODS OF MAKING THE SAME 审中-公开
    确定的抗肿瘤药物及其制备方法

    公开(公告)号:WO2016028851A1

    公开(公告)日:2016-02-25

    申请号:PCT/US2015/045816

    申请日:2015-08-19

    IPC分类号: C07D307/04 C07D307/20

    摘要: Amphipathic amine-esters derived from anhydropentitols are prepared through a short sequence of synthetic steps. The process is initiated by the esterification of an anhydropentitol with a fatty acid chloride or a lipase enzyme to form anhydropentitol fatty acid esters, preferably leaving at least one free hydroxyl. The free hydroxyl group(s) are then sulfonated, forming sulfonated anhydropentitol fatty acid esters. The sulfonyl moiety on the sulfonated anhydropentitol fatty acid esters are then subject to nucleophilic displacement by a hydrophilic moiety, illustrated by a primary amine such as AEE or AEEA. The synthetic pathway is efficient and affords modest to high yields of target amphiphilic compounds, which are useful at least as surfactants and plasticizer substitutes for petroleum derived compounds.

    摘要翻译: 通过短程序的合成步骤制备由脱水三醇衍生的两亲胺 - 酯。 该方法是通过将异氢
    异丙醇与脂肪酰氯或脂肪酶进行酯化反应来形成脱氢异戊醇脂肪酸酯,优选
    留下至少一种游离羟基。 然后将游离羟基磺化,形成磺化的脱水异构醇脂肪酸酯。 然后通过亲水部分对磺化的脱水异构醇脂肪酸酯上的磺酰部分进行亲核置换,如由伯胺如AEE或AEEA所示。 合成途径是有效的,并提供适度的高产量的目标两亲化合物,其至少可用作石油衍生化合物的表面活性剂和增塑剂替代物。