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A novel and efficient amidation of 2-aminothiazole
Authors:Minho Choi  Sun-Woo Won  Hyeju Jo  Mayavan Viji  Seung-Yong Seo  Yeon-Ju Lee  Hyi-Seung Lee  Heesoon Lee  Jin Tae Hong  Young-Shin Kwak  Jae-Kyung Jung
Affiliation:1. College of Pharmacy and Medicinal Research Center (MRC), Chungbuk National University, Cheongju 362-763, Republic of Korea;2. College of Pharmacy, Korea University, Sejong 339-700, Republic of Korea;3. College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon 406-779, Republic of Korea;4. Korea Ocean Res & Dev Inst, Ansan 426-44, South Korea
Abstract:A facile and efficient method has been developed for the synthesis of novel thiazolyl carboxamide derivatives by direct reaction of the corresponding esters and 2-aminothiazole. Treatment of 2-aminothiozole with various carboxylic esters in the presence of t-butylmagnesium chloride provides the biologically significant thiazolyl carboxamide derivatives in good to excellent yields.
Keywords:Amide   2-Aminothiazole   Carboxamide   Transamidation   t-Butylmagnesium chloride
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