83728-52-3Relevant academic research and scientific papers
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors
Lu, Xiang,Zhang, Hui,Li, Xi,Chen, Guo,Li, Qing-Shan,Luo, Yin,Ruan, Ban-Feng,Chen, Xian-Wei,Zhu, Hai-Liang
experimental part, p. 6827 - 6832 (2012/02/02)
A series of pyridine acyl sulfonamide derivatives (1-24) have been designed and synthesized and their biological activities were also evaluated as potential cyclooxygenase-2 (COX-2) inhibitors. Among all the compounds, compound 23 displayed the most poten
TiCl4-promoted direct N-acylation of sulfonamide with carboxylic ester
Fu, Shaomin,Lian, Xiaoyan,Ma, Tongmei,Chen, Wenhua,Zheng, Meifang,Zeng, Wei
supporting information; experimental part, p. 5834 - 5837 (2010/11/04)
Several Lewis acids were investigated as promoters in the intermolecular or intramolecular direct N-acylation reaction of sulfonamides using carboxylic ester as an acylating agent. TiCl4 was found to possess the highest activity and enhanced efficiently sulfonamide to form N-acylsulfonamides under optimized conditions. This method provides a novel approach to make N-acylsulfonamides from ester via an easy work-up procedure.
Potential Acyl-transfer Agents. Reactions of N-Acyl-2-pyridinecarboxamides with Nucleophiles
Morkved, Eva H.,Cronyn, Marshall W.
, p. 381 - 388 (2007/10/02)
A fast reaction is obserwed between a series of N-acyl-2-pyridinecarboxamides and cyclopentylamine or pyrrolidine.Most of the acylamides react exclusively at the pyridine-2-carbonyl group.The selectivity of these reactions is explained by the reaction of the pyridine-nitrogen as a base towards the external nucleophile in a five-ring transition state.The acylamides undergo slow reactions with 4-methylaniline, methanol or water.Several reaction paths are observed with these less reactive nucleophiles.An intramolecular acyl group transfer prior to the reaction with an external nucleophile is indicated for three of the N-acylamides which have an N,N-dialkylamino substituent in the pyridine-4-position.Nucleophilic attack occurs predominantly at the N-acyl group of these three compounds which are moderately active acyl-transfer agents.
