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Microwave-Assisted Synthesis of 5-Substituted 2-Aminothiophenes Starting from Arylacetaldehydes

Germain Revelant, Sandrine Dunand, Stéphanie Hesse*, Gilbert Kirsch

*Laboratoire d'Ingénierie Moléculaire et Biochimie Pharmacologique, Institut Jean Barriol, FR CNRS 2843, 1 Boulevard Arago, 57070 Metz, France, Email:

G. Revelant, S. Dunand, S. Hesse, G. Kirsch, Synthesis, 2011, 2935-2940.

DOI: 10.1055/s-0030-1261032

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An easy three-step pathway enabled the synthesis of arylacetaldehydes from the corresponding carboxylic acids in very high yields. A subsequent microwave-assisted Gewald reaction gives 5-substituted-2-aminothiophenes in short time, with high yields and purities.

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Key Words

Gewald reaction, 5-substituted-2-aminothiophenes, thiophenes, microwave synthesis, arylacetaldehydes

ID: J66-Y2011-2640