An Efficient Greener Approach for N-Acylation of Amines in Water Using Benzotriazole Chemistry

利用苯并三唑化学在水中高效、绿色地进行胺的N-酰化反应

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Abstract

A straightforward, mild and cost-efficient synthesis of various arylamides in water was accomplished using versatile benzotriazole chemistry. Acylation of various amines was achieved in water at room temperature as well as under microwave irradiation. The developed protocol unfolds the synthesis of amino acid aryl amides, drug conjugates and benzimidazoles. The environmentally friendly synthesis, short reaction time, simple workup, high yields, mild conditions and free of racemization are the key advantages of this protocol.

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