Dichloromeldrum’s Acid (DiCMA): A Practical and Green Amine Dichloroacetylation Reagent

Dichloromeldrum’s acid is introduced as a bench-stable, nonvolatile reagent for the dichloroacetylation of anilines and alkyl amines to produce α,α-dichloroacetamides, which are important motifs for medicinal chemistry. Products are formed in good to excellent yields with reagent grade solvents, and...

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Bibliographic Details
Published in:Organic letters 2021-05, Vol.23 (9), p.3368-3372
Main Authors: Heard, David M, Lennox, Alastair J. J
Format: Article
Language:English
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Summary:Dichloromeldrum’s acid is introduced as a bench-stable, nonvolatile reagent for the dichloroacetylation of anilines and alkyl amines to produce α,α-dichloroacetamides, which are important motifs for medicinal chemistry. Products are formed in good to excellent yields with reagent grade solvents, and, as the only byproducts are acetone and CO2, no column chromatography is required. Thus, this reagent is practical, efficient, and green for the dichloroacetylation of primary amines.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.1c00850