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The synthesis of 2-substituted azoles through a one-pot three-component reaction

✍ Scribed by Yijun Deng; Dennis J. Hlasta

Publisher
Elsevier Science
Year
2002
Tongue
French
Weight
87 KB
Volume
43
Category
Article
ISSN
0040-4039

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✦ Synopsis

We have discovered a new reaction whereby 2-substituted azoles are formed in the reaction of an azolium ylide with reactive carbonyl compounds. These products contain a leaving group in the a-position, which on solvolysis in the presence of nucleophiles yield azoles with a variety of a-substituents. We have developed new aspects of this chemistry and expanded the scope to include imidazoles, thiazoles, benzimidazoles and triazoles, such that in two reaction steps a wide diversity of substitution patterns are obtained.

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## Abstract magnified image A facile and rapid synthesis of the title compounds via one‐pot reaction of 2‐aminobenzonitrile, orthoesters and ammonium acetate under solvent‐free and microwave condition is described.