Leggio Antonella, Bagalà Jessica, Belsito Emilia Lucia, Comandè Alessandra, Greco Marianna, Liguori Angelo
Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria Edificio Polifunzionale, 87036, Arcavacata, CS, Italy.
Chem Cent J. 2017 Sep 15;11(1):87. doi: 10.1186/s13065-017-0318-9.
A general procedure for the synthesis of amides via the direct condensation of carboxylic acids and amines in the presence of TiCl is reported. The amidation reaction was performed in pyridine at 85 °C with a wide range of substrates providing the corresponding amide products in moderate to excellent yields and high purity. The reaction proceeds with low yields when both the carboxylic acid and the amine are sterically hindered. The process takes place with nearly complete preservation of the stereochemical integrity of chiral substrates.
报道了一种在TiCl存在下通过羧酸和胺直接缩合合成酰胺的通用方法。酰胺化反应在吡啶中于85℃进行，使用多种底物，以中等至优异的产率和高纯度得到相应的酰胺产物。当羧酸和胺在空间上都受阻时，反应产率较低。该过程在手性底物的立体化学完整性几乎完全保留的情况下进行。
