Convenient and efficient access to tri- and tetra-substituted 4-fluoropyridines viaa [3+2]/[2+1] cyclization reaction

Autor: Tang, Xuejiao, Liu, Kun, Qu, Zeming, Zhan, Junyan, Zhu, Rukui, Teng, Fan, Meng, Lili, Huang, Yanmin, Huang, Chusheng, He, Yimiao, Zhu, Qiang
Zdroj: Chinese Chemical Letters; 20220101, Issue: Preprints
Abstrakt: A [3 + 2]/[2 + 1] cycloaddition reaction of gem‑difluorocyclopropenes is presented, offering a mild and efficient approach to accessing tri- and tetra-substituted 4-fluoropyridines in moderate to good yields with excellent regioselectivity. Multiple synthetic applications, including process-scale reactions, modification of bioactive molecules, derivatization reactions and synthesis of the analogue of the PKM2 modulator, are subsequently described.
Databáze: Supplemental Index