Department of Chemistry , University of Delhi , Delhi 110007 , India.
Org Lett. 2019 Jul 5;21(13):5059-5063. doi: 10.1021/acs.orglett.9b01649. Epub 2019 Jun 14.
Metal-free regioselective hydration of o-alkynylaldehydes with the assistance of neighboring carbonyl oxygen is disclosed. The developed protocol provides a facile route to synthesize a series of multisubstituted carbonyl containing scaffolds that enable the potential application toward the synthesis of highly diversified 5-azaindoles. γ-Carbolines and 2,8-diazacarbazoles can also be accessed directly without isolating the dicarbonyl compounds. The developed methodology is operationally simple and environment-friendly, tolerates a wide variety of functional groups, and is applicable toward large scale synthesis.
本文报道了一种在邻位羰基氧的协助下实现邻炔基醛的区域选择性无金属水合的方法。所开发的方法为合成一系列多取代的羰基化合物提供了一种简便的途径，这些化合物为高度多样化的 5-氮吲哚的合成提供了潜在的应用。γ-咔啉和 2,8-二氮杂咔唑也可以直接得到，无需分离二羰基化合物。该方法操作简单、环境友好，对各种官能团具有良好的耐受性，并且适用于大规模合成。
