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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 54, Number 4
JKCSEZ 54(4)
August 20, 2010 

 
Title
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

마이크로웨이브 조사와 Diisopropylcarbodiimide (DIC)/7-Aza-1-hydroxybenzotriazole
(HOAt): N-Protected Amino Acid와 Hydrazine으로부터
다양한 Hydrazide합성을 위한 반응조건
Author
Mona Albatal, Mohamad Abdul Ghani, Ayman El Faham*, Hassan M Al Hazimi, Hassan H Hammud

Mona Albatal, Mohamad Abdul Ghani, Ayman El Faham*, Hassan M Al Hazimi, Hassan H Hammud
Keywords
Microwave irradiation, Carbodiimide, 7-Aza-1-hydroxybenzotriazole, Amino acid hydrazide, Peptide hydrazide , Microwave irradiation, Carbodiimide, 7-Aza-1-hydroxybenzotriazole, Amino acid hydrazide, Peptide hydrazide
Abstract

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).

Page
419 - 428
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