Electrophilic Activation of Carboxylic Anhydrides for Nucleophilic Acylation Reactions
Varun Kumar, Anil Rana, Chhuttan Lal Meena, Nidhi Sharma, Yashwant Kumar, Dinesh Mahajan*
*Drug Discovery Research Center, Translational Health Science and Technology Institute, Faridabad 121001, India, Email: dinesh.mahajanthsti.res.in
V. Kumar, A. Rana, C. L. Meena, N. Sharma, Y. Kumar, D. Mehajan, Synthesis, 2018, 50, 3902-3910.
DOI: 10.1055/s-0037-1609564 (free Supporting Information)
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Electrophilic activation of carboxylic anhydride using methanesulfonyl chloride is an efficient method for nucleophilic acylation, which increases product yield by restricting the formation of corresponding acid as a side product. The developed protocol enables one-pot nucleophilic acylation of anhydrides with several types of N- and S-nucleophiles in high yield demonstrating appreciable functional group tolerance.
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nucelophilic acylation, amides, electrophilic activation, anhydride activation, mesyl chloride