7504-69-0Relevant articles and documents
Method for synthesizing amide compound through photocatalysis in water phase
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Paragraph 0072-0075, (2019/10/01)
The invention discloses a method for synthesizing an amide compound through photocatalysis in a water phase. The method comprises the following steps: putting catalysis amounts of a free radical initiator, an amine derivative, a carboxylic acid derivative, a phase transfer catalyst, an inorganic base and water into a reaction container, carrying out a reaction in a photocatalysis reaction instrument at certain power under a room temperature condition, after a certain time, carrying out extraction by using a small amount of ethyl acetate, and carrying out recrystallization, so as to obtain theamide compound, wherein the free radical initiator is eosin, methyl orange, sodium persulfate, ammonium persulfate or potassium peroxodisulfate, the phase transfer catalyst is tetrabutylammonium bromide, and the power of the photocatalytic reaction instrument is 5W. By adopting the method disclosed by the invention, toxic thionyl chloride or phosphorus oxychloride is not needed for a chlorinationreaction, water is adopted as a solvent, a novel photocatalysis method is used, and the amide compound with a high yield can be prepared through a room-temperature reaction for 2-5 hours with an incandescent light bulb of 5W, and in addition, the method is simple in aftertreatment, and low in cost and is an ideal green synthesis method of amide compounds.
Method for synthesizing N-aryl aromatic amide by adopting aromatic hydrazine
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Paragraph 0104-0107, (2018/03/26)
The invention discloses a method for synthesizing N-aryl aromatic amide by adopting aromatic hydrazine. The method includes that arylboronic acid, the aromatic hydrazine, a primary catalyst and an auxiliary catalyst are added in a solvent, the N-aryl aromatic amide as is indicated in the formula III is obtained by performing separation and purification after heating reflux reaction, and CO is fedto a reaction to enable pressure of the reaction system to be 0.1-5MPa during reaction. The method is concise and efficient, phenylhydrazine is substituted, organic boronic acid and CO which are stable in air and easy to obtain are taken as raw materials, metal palladium is taken as the primary catalyst, copper or iron is taken as the auxiliary catalyst, and the N-aryl aromatic amide is synthesized efficiently under mild reaction conditions.
Anticonvulsant activity of some 4-methoxy- and 4-chlorobenzanilides
Clark,McMillian
, p. 220 - 222 (2007/10/02)
A series of mono-, di-, and trimethylated derivatives of 4-chloro- and 4-methoxybenzanilide was synthesized and evaluated for anticonvulsant activity. This series was prepared in the course of studies designed to examine the relationship between anticonvulsant effects and benzamide structure. The compounds were tested in mice against seizures induced by maximal electroshock (MES) and pentylenetetrazole (scMet), as well as with the rotorod assay for neurologic deficit. In mice dosed intraperitoneally, 4-methoxy-2, 6-dimethylbenzanilide (4) showed a median anticonvulsant potency (ED50) of 18.58 mg/kg in the MES test and a median toxicity (TD50) of 133.72 mg/kg in the rotorod toxicity assay, yielding a protective index (PI = TD50/ED50) of 7.2. In mice dosed orally with 4, the anti-MES ED50 was 27.40 mg/kg and the TD50 dose was determined to be 342.58 mg/kg, resulting in a protective index of 12.5.
