Highly efficient and safe procedure for the synthesis of aryl 1,2,3-triazoles from aromatic amine in a continuous flow reactor

• Federica Stazi ^a
• Damiano Cancogni ^a
• Lucilla Turco ^b
• Pieter Westerduin ^a
• Sergio Bacchi ^a

• ^a GlaxoSmithKline Spa, Chemical Development Department, Synthetic Chemistry, Via Fleming 4, 37135 Verona, Italy
• ^b GlaxoSmithKline Spa, Analytical Chemistry, Via Fleming 4, 37135 Verona, Italy

The Letter reports a safe and reliable synthesis of aryl 1,2,3-triazoles from the corresponding anilines via intermediate aryl azides, using a continuous process. The method was applied to a variety of substrates with good to excellent yields, without the need to isolate the reactive and possibly unstable intermediates which were constantly kept at low concentration in the matrix environment.

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