22106-33-8Relevant articles and documents
Pharmacophore mapping, molecular docking, chemical synthesis of some novel pyrrolyl benzamide derivatives and evaluation of their inhibitory activity against enoyl-ACP reductase (InhA) and Mycobacterium tuberculosis
Joshi, Shrinivas D.,Dixit, Sheshagiri R.,Basha, Jeelan,Kulkarni,Aminabhavi, Tejraj M.,Nadagouda, Mallikarjuna N.,Lherbet, Christian
, p. 440 - 453 (2018)
In an effort to produce new lead antimycobacterial compounds, herein we have reported the synthesis of a sequence of new pyrrolyl benzamide derivatives. The new chemical entities were screened to target enoyl-ACP reductase enzyme, which is one of the key enzymes of M. tuberculosis that are involved in type II fatty acid biosynthetic pathway. Compound 3q exhibited H-bonding interactions with Tyr158, Thr196 and co-factor NAD+ that binds the active site of InhA. All the pyrrolyl benzamide compounds were evaluated as inhibitors of M. tuberculosis H37Rv as well as inhibitors of InhA. Among them, few representative compounds were tested for mammalian cell toxicity on the human lung cancer cell-line (A549) and MV cell line that presented no cytotoxicity. Five of these compounds exhibited a good activity against InhA.
Palladium-catalyzed carbonylative synthesis of acylstannanes from aryl iodides and hexamethyldistannane
Chen, Bo,Franke, Robert,Wu, Xiao-Feng,Xu, Jian-Xing,Yuan, Yang
, (2020/07/21)
In this communication, we describe a new method for the carbonylative synthesis of acylstannanes from aryl iodides and hexamethyldistannane. With Pd(PPh3)4 as the catalyst and toluene as the solvent at 60 °C under 10 bar CO for 16 h, the desired acylstannanes were obtained in good to excellent yields. In order to facilitate isolation and analysis, the obtained acylstannanes were transformed into the corresponding benzoic acids by simply stirring under air for 5 h.
Nickel-catalyzed carboxylation of aryl iodides with lithium formate through catalytic CO recycling
Fu, Ming-Chen,Fu, Yao,Shang, Rui,Wu, Ya-Nan
supporting information, p. 4067 - 4069 (2020/04/20)
A protocol for the Ni-catalyzed carboxylation of aryl iodides with formate has been developed with good functional group compatibility for the synthesis of a variety of aromatic carboxylic acids under mild conditions. The reaction tolerates other functionalities for cross-coupling, such as aryl bromide, aryl chloride, aryl tosylate, and aryl pinacol boronate. The reaction proceeds through a carbonylation process with in situ generated carbon monoxide in the presence of a catalytic amount of acetic anhydride and lithium formate, avoiding the use of gaseous CO. The strategy of CO recycling in catalytic amounts is critical for the success of the reaction.
