Propylphosphonic acid anhydride–mediated amidation of Morita–Baylis–Hillman–derived indolizine-2-carboxylic acids
作者:Khethobole C Sekgota、Michelle Isaacs、Heinrich C Hoppe、Ronnett Seldon、Digby F Warner、Setshaba D Khanye、Perry T Kaye
DOI:10.1177/1747519820987156
日期:2021.7
Propylphosphonic acid anhydride has been successfully used as a coupling agent in the synthesis of a series of indolizine-2-carboxamido derivatives from indolizine-2-carboxylic acid and its 3-acetylated analogue. The acid substrates were obtained by saponification of the corresponding methyl esters produced, in turn, selectively and efficiently, by time-controlled cyclisation of a single Morita–Baylis–Hillman
丙基膦酸酐已成功地用作偶联剂,由吲哚并嗪-2-羧酸及其3-乙酰化类似物合成了一系列吲哚并嗪-2-羧酰胺基衍生物。酸性底物是通过对相应的甲酯进行皂化而得到的,而相应的甲酯是通过单个Morita-Baylis-Hillman加合物的时间控制环化而选择性而有效地获得的。具有药用潜力的各种氨基和肼基化合物已被用于制备吲哚嗪-2-甲酰胺基和肼基衍生物。