The synthesis of 2-(5-methyl-2-nitrophenyl)-5-(substituted)-1,3,4-oxadiazoles (5a-e) and thiadiazoles (6a-e) was carried out by refluxing of N-(5-methyl-2-nitrobenzoyl)-2-substituted carbohydrazide with phosphorous oxychloride and Lawesson's reagent respectively. The N-(5-methyl-2-nitrobenzoyl)-2-substituted carbohydrazides was synthesized by treating 2(5-methyl-2-nitrobenzohydrazide) with various aryl acids in the presence of HATU and DIPEA. Compounds 6a, 5c and 5d exhibited significant cytotoxic properties when compared to standard podophyllotoxin. Further, the compounds were also studied for their antibacterial activities.
Although the first synthesis of benzotriazole was performed in the 19th century still new methods for their preparation have developed. In this micro review authors focus mostly on the various synthetic strategies developed so far to synthesize benzotriazole and its derivatives by different strategies, such as metal‐free, metal‐assisted [3 + 2] cycloaddition reactions, cyclocondensations, flow methods, heterocyclizations, and so forth. This micro review combines recent (2005–2022 till date) information on the strategies used for the synthesis of benzotriazoles. Moreover, a brief overview of the bio applications of the benzotriazole scaffold along with pharmacological activity is also discussed.
A facile, one-pot, and proficient method was developed for the production of various 2-arylaminobenzimidazoles. This methodology is based for the first time on a copper catalyst promoted domino C–N cross-coupling reaction for the generation of 2-arylaminobenzimidazoles. Mechanistic investigations revealed that the synthetic pathway involves a copper-based desulphurization/nucleophilic substitution and a subsequent domino intra and intermolecular C–N cross-coupling reactions. Some of the issues typically encountered during the synthesis of 2-arylaminobezimidazoles, including the use of expensive catalytic systems and the low reactivity of bromo precursors, were addressed using this newly developed copper-catalyzed method. The reaction procedure is simple, generally with excellent substrate tolerance, and provides good to high yields of the desired products.
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