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Abbas Haruna Umar

As seen in: ACS Publications
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Articles

Reappraising Dichloromethane: Uncovering a Hidden Coupling Reagent for Activating Carboxylic Acids in Direct Amide Synthesis Click to copy article link Article link copied!

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By Nithin Pootheri, Sunwoo Lee, Abbas Haruna Umar
| ACS Publications
After optimizing conditions, we investigated the range of carboxylic acid substrates using benzylamine as the nucleophile ( Scheme 1 A). Among aryl carboxylic acids, electron-donating substituents, such as methyl at meta or para positions, para tert -butyl, methoxy, methylthio, or diphenylphosphino groups, were well tolerated, yielding amide products ( 4 – 11 ) at 61%–78%. 2-Naphthoic, biphenyl-4-carboxylic, and 9-fluorenone-2-carboxylic acids also formed amides ( 12–14 ) in 63%–72% yield.
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