Chen Xue-Bing, Wang Xue-Quan, Song Jia-Na, Yang Qing-Li, Huang Chao, Liu Wei
Key Laboratory of Natural Pharmaceutical and Chemical Biology of Yunnan Province, School of Science Honghe, University Mengzi, Yunnan 661100, China.
Org Biomol Chem. 2017 May 3;15(17):3611-3615. doi: 10.1039/c7ob00306d.
A novel and highly efficient protocol has been developed for the regioselective synthesis of 2-iminothiazole derivatives with potential biochemical interest by the reaction of enaminones, potassium thiocyanate (KSCN), and N-bromo succinimide (NBS) under mild conditions. The reaction proceeds via the formation of α-bromo enaminones as a versatile intermediate followed by thiocyanation/intramolecular cyclization in a one pot manner. The developed method is particularly attractive due to various advantages including operational simplicity, mild conditions, being catalyst free, and high bond-forming efficiency. The proposed protocol explores the synthetic routes of thiazoles by using various functional enaminones.
通过烯胺酮、硫氰酸钾（KSCN）和N-溴代琥珀酰亚胺（NBS）在温和条件下反应，开发了一种新颖且高效的方法用于区域选择性合成具有潜在生化意义的2-亚氨基噻唑衍生物。该反应通过形成α-溴代烯胺酮这一通用中间体进行，随后以一锅法进行硫氰化/分子内环化。所开发的方法具有多种优势，包括操作简单、条件温和、无需催化剂以及高成键效率，因而特别具有吸引力。所提出的方法通过使用各种官能化烯胺酮探索了噻唑的合成路线。
