Wang Ning, Yang Qin, Deng Zhihong, Mao Xuechun, Peng Yiyuan
Key Laboratory of Functional Small Organic Molecules, Ministry of Education, Jiangxi Province's Key Laboratory of Green Chemistry, Jiangxi Normal University, Nanchang 330022, China.
ACS Omega. 2020 Jun 15;5(24):14635-14644. doi: 10.1021/acsomega.0c01344. eCollection 2020 Jun 23.
An efficient method for the synthesis of 2-(-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.
开发了一种高效合成2-（-单氟烯基芳基）喹唑啉酮衍生物的方法。在此背景下，喹唑啉酮环作为内在导向基团，对甲苯磺酸2,2-二氟乙烯酯用作单氟烯烃合成子，通过铑（III）催化的2-芳基喹唑啉酮的C-H键二氟乙烯基化反应，以65-92%的产率得到相应的含单氟烯烃的喹唑啉酮。该方法具有广泛的合成实用性、温和的条件和高效率的特点。
