Song Jinhua J, Reeves Jonathan T, Gallou Fabrice, Tan Zhulin, Yee Nathan K, Senanayake Chris H
Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Old Ridgebury Road/P.O. Box 368, Ridgefield, CT 06877-0368, USA.
Chem Soc Rev. 2007 Jul;36(7):1120-32. doi: 10.1039/b607868k. Epub 2007 Feb 2.
Azaindoles (also called pyrrolopyridines) constitute essential subunits in many pharmaceutically important compounds. The synthesis of azaindoles has been a great synthetic challenge for chemists. Many classical methods for indole synthesis (such as Fischer and Madelung cyclizations) often cannot be effectively applied to the synthesis of the corresponding azaindoles. In recent years, advances in organometallic chemistry have enabled a number of novel and efficient methodologies for azaindole formation as well as for the further functionalization of azaindole templates. In this tutorial review, we have surveyed the recent development of organometallic chemistry-based methods for azaindole synthesis.
氮杂吲哚(也称为吡咯并吡啶)是许多具有重要药学意义的化合物的关键亚基。氮杂吲哚的合成一直是化学家面临的重大合成挑战。许多经典的吲哚合成方法(如费歇尔和马德隆环化反应)往往不能有效地应用于相应氮杂吲哚的合成。近年来,有机金属化学的进展使得一些新颖且高效的方法得以用于氮杂吲哚的形成以及氮杂吲哚模板的进一步官能化。在本教程综述中,我们考察了基于有机金属化学的氮杂吲哚合成方法的最新进展。