- Method for preparing aryl primary amide by adopting metal-catalyzed one-pot method
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The invention discloses a method for synthesizing aryl primary amide by adopting a metal-catalyzed one-pot method. The method comprises the steps of: taking aryl bromidess as raw materials, allowing the aryl bromidess to react with a cyanide source under the action of a palladium catalyst, substituting bromine on an aromatic ring with cyano to obtain cyano aromatic hydrocarbon, directly adding anaqueous solution of alkali into the reaction solution without aftertreatment, and carrying out hydrolysis reaction to obtain aryl primary amide. Compared with the prior art, the method for preparing aryl primary amide from the aryl bromides has the advantages of the short synthesis route, fewer reaction steps, simple operation, mild conditions, the high conversion rate, low toxicity and industrialproduction potential.
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Paragraph 0035; 0036
(2020/04/06)
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- New synthesis method of 2-amino-3-methylpyridine
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The invention belongs to the field of organic substance synthesis and particularly relates to a new synthesis method of 2-amino-3-methylpyridine. With H2O2 being an oxidant, 2-cyano-3-methylpyridine is subjected to incomplete hydrolysis to form 3-methyl-2-pyridinecarboxamide under diluted alkali conditions; then Hofmann degradation is carried out by using fresh sodium hypobromite. The new preparation method not only is reduced in cost and protects environment, but also is simple in operation and convenient in post-treatment. The method is high in yield, is simple in synthesis and is suitable for industrial production.
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Page/Page column 3-4
(2019/05/15)
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- Transition-metal-free synthesis of primary to tertiary carboxamides: A quick access to prodrug-pyrazinecarboxamide
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One-pot expedient and direct carbamoylation of heterocyclics is described. The transformation is realized via direct dehydrogenative aminocarbonylation of heterocyclic compounds under transition-metal-free conditions. This method is regioselective and the protocol is proved to be scalable on a gram scale. Further, the therapeutically useful antitubercular agent pyrazinecarboxamide is successfully synthesized by employing this protocol.
- Mete, Trimbak B.,Singh, Ankit,Bhat, Ramakrishna G.
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supporting information
p. 4709 - 4712
(2017/11/21)
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- Efficient Mo(VI)-catalyzed hydration of nitrile with acetaldoxime
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A method for the selective hydration of nitrile to amide by employing commercially available acetaldoxime and inexpensive oxometallate such as molybdate, vanadate, and tungstate in environmentally friendly water is described. Under this protocol, nitriles including aromatic nitriles, heterocyclic nitriles, and aliphatic nitriles were converted into the corresponding amides in good to excellent yields.
- Ma, Xiaoyun,He, Ying,Lu, Ming
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supporting information
p. 474 - 480
(2014/01/23)
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- SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to compounds that can modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
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Page/Page column 74; 75
(2013/08/28)
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- The hydration of nitriles catalyzed by simple transition metal salt of the fourth period with the aid of acetaldoxime
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We describe here a method for selective hydration of nitriles into the corresponding amides by employing commercially available acetaldoxime and simple transition metal catalysts such as nickel salts, zinc salts, cobalt salts and manganese salts in water. Nickel salts show the highest catalytic activity, owing to their relatively small diameter of the metal cation. Nitriles having electron-withdrawing groups could be converted into the corresponding amides in excellent yields using nickel catalyst at room temperature. Heterocyclic nitriles with heteroatom lone pair positioned ortho to the nitrile group show high reactivity; even these special nitriles could be hydrated by transition metal catalyst and water at refluxing temperature in the absence of acetaldoxime. Copyright
- Ma, Xiaoyun,He, Ying,Wang, Pengcheng,Lu, Ming
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experimental part
p. 377 - 382
(2012/08/08)
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