Zhang Yanqiu, Zhang Zhiliang, Xia Yunxin, Wang Jiayi, Peng Yanqing, Song Gonghua
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China.
J Org Chem. 2023 Sep 15;88(18):12924-12934. doi: 10.1021/acs.joc.3c00760. Epub 2023 Aug 29.
A facile new method for the synthesis of 3,3-disubstituted phthalides is reported. A successive reaction process begins with the TfOH-catalyzed cyclization of -alkynylbenzoic acids followed by an -regioselective electrophilic alkylation of various electron-rich aromatic compounds or alkenes, which has been successfully developed. The corresponding regioselective products of 3-substituted phthalide were obtained in good to high yields.
报道了一种简便的合成3,3-二取代苯酞的新方法。已成功开发出一种连续反应过程，该过程始于三氟甲磺酸催化的α-炔基苯甲酸环化反应，随后是各种富电子芳香化合物或烯烃的α-区域选择性亲电烷基化反应。以良好至高收率得到了相应的3-取代苯酞区域选择性产物。
