Advanced Research Institute and Department of Chemistry, Taizhou University, 1139 Shifu Avenue, Taizhou 318000, P.R. China.
J Org Chem. 2021 Mar 19;86(6):4646-4660. doi: 10.1021/acs.joc.0c03041. Epub 2021 Mar 8.
A [3 + 2]-annulation of -difluoroalkenes and pyridinium ylides was developed employing ambient air as the sole oxidant in an open-vessel manner, affording a series of multifunctionalized 2-fluoroindolizines in moderate to good yields. In this reaction, -difluoroalkene acts as a C2 synthon and entirely avoids the competitive addition-elimination process, which provides facile access to 2-fluoroindolizines.
开发了一种在开放容器中以环境空气作为唯一氧化剂的[3+2]环化反应，使 -二氟烯烃和吡啶翁叶立德发生反应，以中等至良好的收率得到一系列多功能化的 2-氟吲哚嗪。在这个反应中，-二氟烯烃充当 C2 合成子，完全避免了竞争的加成-消除过程，这为 2-氟吲哚嗪的制备提供了简便的途径。
