37009-55-5Relevant academic research and scientific papers
Synthesis method of alpha-acylamino ketone compound
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Paragraph 0027-0029; 0030-0032; 0050, (2020/12/08)
The invention discloses a synthesis method of an alpha-acylamino ketone compound, and belongs to the technical field of organic synthesis. The preparation method comprises the following steps: mixingan alkenyl azide compound 1, a carboxylic acid compound 2 and an organic solvent, and heating to react to obtain the alpha-acylamino ketone compound 3. Compared with the prior art, the method has thefollowing advantages: (1) the synthesis process is simple and efficient, no catalyst is needed in the whole process, and the alpha-acylamino ketone compound can be obtained with high yield by dissolving the alkenyl azide compound and the carboxylic acid compound in the solvent and stirring; (2) raw materials are cheap and easy to obtain, reaction conditions are mild, and operation is simple; (3) the substrate is wide in application range and can be used for modifying drug molecules; and (4) the atom economy is high, and the requirements of green chemistry are met.
Synthesis of α-Amidoketones through the Cascade Reaction of Carboxylic Acids with Vinyl Azides under Catalyst-Free Conditions
Gao, Cai,Zhou, Qianting,Yang, Li,Zhang, Xinying,Fan, Xuesen
, p. 13710 - 13720 (2020/11/13)
An efficient synthesis of α-amidoketone derivatives through the cascade reactions of carboxylic acids with vinyl azides is presented. Compared with literature protocols, notable features of this new method include catalyst-free conditions, broad substrate scope, good tolerance of a wide range of functional groups, and high efficiency. In addition, the synthetic potential of this method as a tool for late-stage modification was convincingly manifested by its application in the structural elaborations of a number of carboxylic acid drug molecules.
