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
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).
Albatal, Mona,Ghani, Mohamad Abdul,El-Faham, Ayman,Al-Hazimi, Hassan M.,Hammud, Hassan H.
experimental part
p. 419 - 428
(2010/11/04)
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