Chemo- and Regioselective Alkylation of Pyridine <i>N</i>-Oxides with Titanacyclopropanes
作者:Li-Chen Xu、Xiao-Di Ma、Kun-Ming Liu、Xin-Fang Duan
DOI:10.1021/acs.orglett.3c03469
日期:2023.12.8
herein they react preferentially with pyridine N-oxide to accomplish C2–H alkylation beyond these functionalities with double regioselectivity. After being pyridylated at the less hindered C–Ti bond, the remaining C–Ti bond of titanacyclopropanes can be further functionalized by various electrophiles, allowing facile introduction of complex alkyls onto the C2 of pyridines. Its synthetic potential has been
虽然环丙烷钛主要用于与酯、酰胺和氰基反应进行环丙烷化,但在此它们优先与吡啶N-氧化物反应以完成除这些官能团之外的具有双区域选择性的C2-H烷基化。在受阻较小的 C-Ti 键处被吡啶基化后,环丙烷中剩余的 C-Ti 键可以通过各种亲电子试剂进一步官能化,从而可以轻松地将复杂的烷基引入到吡啶的 C2 上。其合成潜力已通过药物的后期多样化得到证明。