Rhodium-Catalyzed Merging of 2-Arylquinazolinone and 2,2-Difluorovinyl Tosylate: Diverse Synthesis of Monofluoroolefin Quinazolinone Derivatives

Rhodium-Catalyzed Merging of 2-Arylquinazolinone and 2,2-Difluorovinyl Tosylate: Diverse Synthesis of Monofluoroolefin Quinazolinone Derivatives
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铑催化 2-芳基喹唑啉酮和 2,2-二氟乙烯基甲苯磺酸酯的合并:单氟烯烃喹唑啉酮衍生物的多样化合成

DOI:
10.1021/acsomega.0c01344
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发表时间:
2020-06
期刊:
影响因子:
4.1
通讯作者:
Peng Yiyuan
Peng Yiyuan
中科院分区:
化学3区
文献类型:
--
作者:
Wang Ning;Yang Qin;Deng Zhihong;Mao Xuechun;Peng Yiyuan

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发展了一种合成2-(邻单氟烯基芳基)喹唑啉酮衍生物的有效方法。以喹唑啉酮环为导向基团,2,2-二氟乙烯基甲苯磺酸酯为单氟烯烃合成子,在Rh(III)催化下,2-芳基喹唑啉酮与C-H键发生二氟乙烯基化反应,得到相应的含单氟烯烃的喹唑啉酮,产率为65- 92%。该方法具有合成用途广、条件温和、效率高的特点。
An efficient method for the synthesis of 2-(o-monofluoroalkenylaryl)quinazolinone derivatives was developed. In this context, the quinazolinone ring served as the inherent directing group, 2,2-difluorovinyl tosylate was used as the monofluoroolefin synthon, and Rh(III)-catalyzed C–H bond difluorovinylation of 2-arylquinazolinons was performed to give the corresponding monofluoroalkene-containing quinazolinons in yields of 65–92%. The method is characterized by broad synthetic utility, mild conditions, and high efficiency.
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