期刊
CHEMISTRY-AN ASIAN JOURNAL
卷 16, 期 8, 页码 879-889出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/asia.202100151
关键词
Late-stage functionalization; C− H Functionalization; N-(acyloxy)phthalimide; Decarboxylative coupling; Heterocycle
资金
- SERB [ECR/2017/001408]
Synthetic methods enabling late-stage modification of heterocycles are crucial in the pharmaceutical and agrochemical industry. The development of catalysts has made C-H alkylation of heterocycles more accessible and efficient, leading to significant breakthroughs in medicinal chemistry.
Synthetic methods enabling late-stage modification of heterocycles hold tremendous importance in the pharmaceutical and agrochemical industry and drug discovery. Accordingly, efficient, functional group tolerant and selective late-stage alkylation of valuable molecular entities is of enormous significance and well-acknowledged in medicinal chemistry. Radical alkylation of heteroarenes employing carboxylic acids as the alkyl radical precursor represents one of the most direct ways of C-H functionalizations of heterocycles. Recently, the field has undergone a revolutionary development especially with regard to the generation of alkyl radicals under much milder conditions. In this regard N-(acyloxy)phthalimides (NHPI esters) have emerged as a suitable precursor of a diverse set of alkyl radicals allowing formal C-H alkylation of not only N-heteroarenes but a diverse set of non-aromatic heterocycles under visible light photocatalysis or electrochemical conditions. This review delineates all these discoveries and provides readers a comprehensive overview of this rapidly expanding field.
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