College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea.
J Org Chem. 2013 Feb 1;78(3):1283-8. doi: 10.1021/jo302590a. Epub 2013 Jan 16.
A new synthetic route to indolizines with various substituents on the pyridine moiety was developed by utilizing a facile cycloaromatization of 2-acetylpyrrole derivatives. Without isolation, the resulting intermediates were allowed to react with various electrophiles to afford a range of indolizines. In particular, Suzuki-Miyaura cross-coupling of O-triflates with (hetero)arylboronic acids permitted introduction of diverse substituents at the C8 position of an indolizine skeleton.
开发了一种新的合成吲哚嗪的方法，通过利用 2-乙酰基吡咯衍生物的简便环芳构化反应，可以在吡啶部分上得到各种取代基的吲哚嗪。无需分离，所得中间体可与各种亲电试剂反应，得到一系列吲哚嗪。特别是，O-三氟甲磺酸酯与（杂）芳基硼酸的铃木-宫浦偶联反应允许在吲哚嗪骨架的 C8 位置引入各种取代基。
