jo8b01460_si_001.pdf (648.06 kB)
Synthesis of Quinazolin-4(3H)‑ones via the Reaction of 2‑Halobenzamides with Nitriles
journal contribution
posted on 2018-08-07, 12:21 authored by Xiaoqiang Yu, Linqi Gao, Linan Jia, Yoshinori Yamamoto, Ming BaoThis
paper describes a convenient method to synthesize quinazolin-4(3H)-ones from simple and readily available 2-halobenzamides
and nitriles. The Lewis acid Cu-catalyzed nucleophilic addition of
2-halobenzamide to nitriles followed by SNAr reaction proceeds
smoothly in the presence of tBuOK as a
base to produce quinazolinone derivatives.