试剂
组合化学
分子内力
化学
环境友好型
串联
连二亚硫酸钠
有机化学
材料科学
生态学
复合材料
生物
作者
Pankaj Gupta,Surabhi Panday,Amitava Hazra,Joydev K. Laha
出处
期刊:ACS Sustainable Chemistry & Engineering
[American Chemical Society]
日期:2023-11-16
卷期号:11 (48): 17031-17037
标识
DOI:10.1021/acssuschemeng.3c05103
摘要
A novel intramolecular direct amidation of unactivated esters with nitroarenes under a mild, practical, and scalable synthetic protocol is the subject of this present investigation. The method uses a green, environmentally friendly, inexpensive, and readily available single-electron reductant, sodium dithionite (Na2S2O4), as the sole reagent under metal-free, additive-free, mild reaction conditions. Various nitroarenes containing ortho-ester functionalities are subjected to tandem chemoselective reductive cyclization/amidation to deliver high-value azaheterocycles in excellent yields. Notably, the present method enables the rapid construction of pharmaceutically relevant azaheterocycles from readily accessible ortho-functionalized nitroarenes. Furthermore, gram-scale synthesis of several key starting materials and pharmaceuticals demonstrates the practical utility of the developed protocol.
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