- Synthesis of α-Amidoketones through the Cascade Reaction of Carboxylic Acids with Vinyl Azides under Catalyst-Free Conditions
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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.
- Gao, Cai,Zhou, Qianting,Yang, Li,Zhang, Xinying,Fan, Xuesen
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p. 13710 - 13720
(2020/11/13)
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- Self-Catalyzed Rapid Synthesis of N-Acylated/ N-Formylated α-Aminoketones and N-Hydroxymethylated Formamides from 3-Aryl-2 H-Azirines and 2-Me/Ph-3-Aryl-2 H-Azirines
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A rapid and effective method has been established for the synthesis of N-acylated α-aminoketone derivatives by the reaction of 3-aryl-2H-azirines and highly substituted 2-Me/Ph-3-aryl-2H-azirines with various carboxylic acids under ambient air within 10 min at room temperature. N-Trifluoroacetylated α-aminoketones with different substituents have been reported in the presence of trifluoroacetic acid. This protocol is equally effective to synthesize N-formylated α-aminoketone and N-hydroxymethylated formamide derivatives.
- De, Aramita,Majee, Adinath,Santra, Sougata,Zyryanov, Grigory V.
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p. 3926 - 3930
(2020/07/14)
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- Synthesis method of alpha-acylamino ketone compound
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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.
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Paragraph 0027-0029; 0030-0032; 0114
(2020/12/08)
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- A Convenient Synthesis of Aminomethyl Ketones (α-Amino Ketones)
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Several N,N-diformylaminomethyl ketones 3 were prepared by treating the respective bromomethylketone 1 with sodium diformylamide in acetonitrile at room temperature.This reaction produced from N-formylaminomethyl ketones 4 when ethanol was used as the solvent.One of the formyl groups of N,N-difomylaminomethyl ketones was selectively removed by using a catalytic amount of sodium or potassium hydroxide in alcohol to the corresponding N-formylaminomethyl ketones 4.The formyl groups of both N,N-diformyl- and N-formylaminomethyl ketones could be easily removed by either5percent hydrochloric acid in ethanol or 6N hydrochloric acid to give the corresponding aminomethyl ketone hydrochlorides 5.These reactions are general and give high yield of the products.
- Yinglin, Han,Hongwen, Hu
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p. 615 - 618
(2007/10/02)
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- A CONVENIENT PREPARATION OF AMINOMETHYL ARYL KETONES AND THEIR DERIVATIVES
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A convenient preparation of N-phenacyl diformamides, N-phenacyl formamides and aminomethyl aryl ketone hydrochlorides from aryl bromomethyl ketones and sodium diformylamide was described.
- Ying-lin, Han,Hong-ven, Hu
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p. 5285 - 5286
(2007/10/02)
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