31733-55-8

Upstream product

• 2945-08-6 methyl (4-nitrophenyl)acetate 
• 100-46-9 benzylamine 
• 50434-36-1 4-nitrophenylacetyl chloride 
• 104-03-0 4-nitrobenzeneacetic acid 

Downstream Products

• 31733-58-1 N-benzyl-2-(4-aminophenyl)acetamide 
• 1612231-86-3 1-benzyl-4-(ethylthio)-3-(4-nitrophenyl)quinolin-2(1H)-one 
• 1612232-18-4 N-benzyl-3,3-bis(ethylthio)-2-(4-nitrophenyl)acrylamide 

Relevant academic research and scientific papers

Amide group-containing compounds and use for cancer treatment

Therapeutic compounds containing a phenyl core and amide link(s). Also described are pharmaceutical compositions incorporating the therapeutic compounds and a method for treating cancer with the compounds. These compounds are cytotoxic to stomach, colon, breast, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.

Pharmaceutical composition and method of treating cancer

Cytotoxic compounds containing a phenyl core, amide link(s), an imidazolinone or a propenamide moiety. Also described are pharmaceutical compositions incorporating the cytotoxic compounds and methods for treating cancer. These compounds are cytotoxic against breast, prostate, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.

Synthetic method for preparing amide compounds through co-catalysis of niobium pentachloride and ionic liquid

The invention relates to a synthetic method for preparing amide compounds through co-catalysis of niobium pentachloride and ionic liquid. The preparation method is characterized by comprising the following steps: weighing organic carboxylic acid, organic amine, niobium pentachloride, ionic liquid and a molecular sieve, adding the materials into a reactor, adding an organic solvent, and reacting for 6-24 hours at the reaction temperature of 70-110 DEG C to obtain a corresponding amide product. The molar ratio of the organic carboxylic acid to the organic amine to the niobium pentachloride to the ionic liquid is 1:(1-3):(0.01-1):(0.05-1); wherein the mass ratio of the organic carboxylic acid to the molecular sieve is 1: (0.2-1). According to the method, the substrate range is expanded, the reaction yield is high (95% or above), the catalyst dosage is small, the atom economy is high, the catalyst is cheap and easy to obtain, the production cost can be greatly reduced, and the method is suitable for industrial production.

Direct amidation of non-activated carboxylic acid and amine derivatives catalyzed by TiCp2Cl2

This paper described a mild and efficient direct amidation of non-activated carboxylic acid and amine derivatives catalyzed by TiCp2Cl2. Arylacetic acid derivatives reacted with different amines to afford the corresponding amides in good to excellent yield except of aniline. Aryl formic acids failed to react with aniline but smoothly reacted with aliphatic amines and benzylamine in moderate to good yield, fatty acids reacting with benzyl and aliphatic amines give amides in good to excellent yield. Chiral amino acids derivatives were transformed into amides without racemization in moderate yield. The possible mechanism of direct amidation catalyzed by TiCp2Cl2 was discussed. This catalytic method is very suitable for the amidation of low sterically hindered arylacetic acid, fatty acids with different low sterically hindered amines except aniline, as well as the amidation of aryl formic acid with benzyl and aliphatic amines.

Air-stable Bis(pentamethylcyclopentadienyl) Zirconium Perfluorooctanesulfonate as an Efficient and Recyclable Catalyst for the Synthesis of N-substituted Amides

Bis(pentamethylcyclopentadienyl) zirconium perfluorooctanesulfonate is an air-stable and water-tolerant Lewis acid. This complex exhibited good thermal stability and high solubility in polar organic solvents. The compound showed relatively strong acidity, with an acid strength of 0.8Ho≤3.3, and high catalytic efficiency for the synthesis of N-substituted amides via the reaction of carboxylic acids with amines, the Ritter reaction of nitriles with alcohols, and the amination of alcohols with amides. Moreover, the complex had good reusability. This catalytic system affords a simple and efficient way to synthesize N-substituted amides.

Palladium-catalyzed c-S activation/aryne insertion/coupling sequence: Synthesis of functionalized 2-quinolinones

The insertion of an aryne into a C-S bond can suppress the addition of an S nucleophile to the aryne in the presence of palladium. Catalyzed by Pd(OAc)2, a wide range of α-carbamoyl ketene dithioacetals readily react with arynes to selectively afford functionalized 2-quinolinones in high yields under neutral reaction conditions by a C-S activation/aryne insertion/intramolecular coupling sequence. The attractive feature of the new strategy also lies in the versatile transformations of the alkythio-substituted quinolinone products. Within range: Under palladium catalysis a wide range of α-carbamoyl ketene dithioacetals readily react with arynes to selectively afford 2-quinolinones in high yields under neutral reaction conditions by the title sequence (see scheme). An attractive feature of the new strategy also lies in the versatile transformations of the alkylthio-substituted quinolinones.

AMIDINE DERIVATIVES WITH NITRIC OXIDE SYNTHETASE ACTIVITIES

Amidine derivative compounds of formula I as defined in the Specification having nitric oxide synthetase inhibitory activity as well as processes for the preparation of and compositions containing said compounds are described

Anticonvulsant activity of some 4-aminophenylacetamides

A series of 4-aminophenylacetamides was prepared and evaluated for anticonsulvant activity. These compounds were prepared during studies designed to determine the relationship between benzamide-like compounds and anticonsulvant effects. Unlike benzamides, these phenylacetamides have a methylene group between the aromatic ring and the amide carbonyl. Consequently, formal conjugation is lost, and the number of conformational degrees of freedom has increased. The compounds were tested in mice against seizures induced by electroshock and pentylenetetrazol, and in the rotorod assay for neurologic deficit. The more active and selective anticonsulvants prepared in this study were those having an additional aromatic ring as part of the substituent on the amide nitrogen. Compound 16, the 4-aminophenylacetamide derived from 2,6-dimethylaniline, was the most potent compound observed (ED50 = 50.50 mg/kg against electroshock-induced convulsions and ED50 = 93.20 mg/kg against pentylenetetrazol-induced convulsions).