Facile synthesis of 2-alkynyl oxazoles via a Ce(OTf)(3)-catalyzed cascade reaction of alkynyl carboxylic acids with tert-butyl isocyanide
Facile synthesis of 2-alkynyl oxazoles via a Ce(OTf)(3)-catalyzed cascade reaction of alkynyl carboxylic acids with tert-butyl isocyanide
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通过 Ce(OTf)(3) 催化的炔基羧酸与叔丁基异氰化物的级联反应轻松合成 2-炔基恶唑
DOI：
10.1039/c9ob02337b
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发表时间：
2020
期刊：
影响因子：
--
通讯作者：
Wang Ying-Chun
中科院分区：
文献类型：
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作者：
Cao Ming;Teng Qing-Hu;Xi Zhi-Wei;Liu Li-Qiu;Gu Ren-Yong;Wang Ying-Chun
我们开发了一种有效的和新的协议，以叔丁基异氰化物和炔基羧酸合成2-炔基恶唑。该方法可以在温和的反应条件下合成多种功能化的恶唑，操作简单，并且这些功能化的恶唑表现出一定的生物活性。化合物2b、2 h、2k、2n、2 p和2 t对人胃癌细胞（MGC 803）和人膀胱癌细胞（T24）具有较好的抗肿瘤活性，IC 50均小于20.0 μM。
We developed an efficient and novel protocol to synthesize 2-alkynyl oxazoles from tert-butyl isocyanide and alkynyl carboxylic acids. This method allowed the synthesis of diversely functionalized oxazoles under mild reaction conditions, coupled with operational simplicity and these functionalized oxazoles showed a certain degree of biological activity. Moreover, compounds 2b, 2h, 2k, 2n, 2p and 2t exhibited good anticancer activities in human gastric cancer cells (MGC803) and human bladder tumor cells (T24), with IC50 below 20.0 μM.