1-甲基-5H-茚[1,2-b]吡啶三氟甲磺酸盐-5-(4-二甲氨基)苄烯衍生物及其制备
申请公布号:CN101948428B
申请号:CN201010223809.2
申请日期:2010.07.06
申请公布日期:2012.06.06
发明人:朱永明;李雯;闻娣娣
分类号:C07D221/16(2006.01)I;A61K31/435(2006.01)I;A61P35/00(2006.01)I;A61P35/02(2006.01)I
主分类号:C07D221/16(2006.01)I
代理人:陶海锋
地址:215123 江苏省苏州市工业园区仁爱路199号
摘要:本发明属于抗肿瘤药物制备领域,具体涉及可以作为DNA拓扑异构酶抑制剂的1-甲基-5H-茚[1,2-b]吡啶三氟甲磺酸盐-5-(4-二甲氨基)苄烯衍生物及其制备方法,包括以下步骤:(1)成盐反应:将5H-茚[1,2-b]吡啶与三氟甲磺酸甲酯以摩尔比1∶2~3的比例,于氮气保护下,室温下搅拌反应获得1-甲基-5H-茚[1,2-b]吡啶三氟甲磺酸盐;(2)偶联反应:将步骤(1)所得1-甲基-5H-茚[1,2-b]吡啶三氟甲磺酸盐与4-二甲氨基苯甲醛以摩尔比1.0∶1.4~1.6,于冰醋酸中回馏制备获得1-甲基-5H-茚[1,2-b]吡啶三氟甲磺酸盐-5-(4-二甲氨基)苄烯衍生物;本发明获得的化合物对白血病细胞和人喉鳞癌细胞具有较强的抑制作用,并且,本发明所述的制备方法工艺简单,产率良好,达到65%左右。
主权项:1.一种1-甲基-5H-茚[1,2-b]吡啶三氟甲磺酸盐-5-(4-二甲氨基)苄烯衍生物,其特征在于,其结构式如下所示:<img file="FSB00000749638400011.GIF" wi="1046" he="502" />式中,R<sub>1</sub>选自H、CH<sub>3</sub>、F、或Cl的一种;R<sub>1</sub>可以连接在6,7,8,9中的任一位置,位置编号如下所示:<img file="FSB00000749638400012.GIF" wi="896" he="521" />
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