三氟甲磺酸银和三氟甲磺酸酐促进的酰化 1-氨基异喹啉的便捷合成。
Silver triflate and triflic anhydride-promoted expedient synthesis of acylated 1-aminoisoquinolines.
作者信息
Li Yuewen, Gao Liang, Zhu Hui, Li Guangming, Chen Zhiyuan
机构信息
Key Laboratory of Functional Small Organic Molecules, Ministry of Education and Key Laboratory of Green Chemistry of Jiangxi Province, College of Chemistry & Chemical Engineering, Jiangxi Normal University, Nanchang, Jiangxi 330022, China.
出版信息
Org Biomol Chem. 2014 Sep 28;12(36):6982-5. doi: 10.1039/c4ob01301h.
A practical and convergent synthesis of biologically active 1-(N-acyl)-1-aminoisoquinolines from the reaction of 2-alkynylbenzaldoximes with amides has been realized. The readily available amides could be activated with triflic anhydride (Tf2O) and could efficiently participate in the domino reaction of 2-alkynylbenzaldoximes when catalyzed by AgOTf, thus providing various acylated 1-aminoisoquinolines with up to 98% yields.
通过2-炔基苯甲醛肟与酰胺的反应，实现了具有生物活性的1-(N-酰基)-1-氨基异喹啉的实用且收敛的合成。容易获得的酰胺可以用三氟甲磺酸酐（Tf2O）活化，并且在AgOTf催化下可以有效地参与2-炔基苯甲醛肟的多米诺反应，从而以高达98%的产率提供各种酰化的1-氨基异喹啉。
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