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KMID : 1059520100540040419
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Journal of the Korean Chemical Society
2010 Volume.54 No. 4 p.419 ~ p.428
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Microwave Irradiation and Diisopropylcarbodiimide (DIC)/7-Aza-1-hydroxybenzotriazole (HOAt): A Potent Combination for Synthesis of Variuos Hydrazide from N-Protected Amino Acid and Hydrazine
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Albatal, Mona
Ghani, Mohamad Abdul
Hammud, Hassan H.
El-Faham, Ayman
Al-Hazimi, Hassan M.
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Abstract
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Here we describe a fast and rapid technique for preparation of amino acid hydrazide as well as peptide hydrazide derivatives using diisopropylcarbodiimide (DIC)/1-hydroxybenzotriazoles (HOXt) (X = A or B) under microwave irradiation employing a multimode reactor (Synthos 3000 Aton Paar, GmbH, 1400 W maximum magnetron). A comparison between conventional and microwave irradiation was described. The microwave methodology is rapid, convenient, proceeds under mild conditions. Diisopropylcarbodiimide (DIC)/7-aza-1-hydroxybenzotriazole (HOAt) always gave much better yield (95 - 98%) and purity than diisopropylcarbodiimide (DIC)/1-hydroxybenzotriazole (HOBt).
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KEYWORD
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Microwave irradiation, Carbodiimide, 7-Aza-1-hydroxybenzotriazole, Amino acid hydrazide, Peptide hydrazide
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