Iodine-catalyzed oxidative annulation: facile synthesis of pyrazolooxepinopyrazolones methyl azaarene sp C-H functionalization.

Org Biomol Chem

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Shandong, Yantai, 264005, P. R. China.

Published: February 2022

An iodine-catalyzed methyl azaarene sp C-H functionalization has been developed for the synthesis of a seven-membered -heterocyclic architecture containing three different heterocyclic aromatic hydrocarbons. This method can be applied to a wide range of substituted methyl azaarenes and diverse 2,4-dihydro-3-pyrazol-3-ones, and brings about the efficient preparation of 2,9-dihydrooxepino[2,3-:6,5-']dipyrazol-3(7)-ones in high yields with the merits of low catalyst loading, good functional group tolerance and metal-free conditions.

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http://dx.doi.org/10.1039/d1ob02436aDOI Listing

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