Convenient synthesis of 2-alkylamino-6-carboxy-5,7-diarylcyclopenteno[1,2-b]pyridines via direct acylamination with imidoyl chlorides

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• 作者：Takahashi ; Hirobumi ; Fukami ; Takehiro ; Kojima ; Hisaki ; Yamakawa ; Takeru ; Takahashi ; Hiroyuki ; et. al.
• 关键词：Acylamination ; Imidoyl chloride ; Cyclopenteno[1 ; 2-b]pyridines ; ETA antagonist
• 刊名：Tetrahedron
• 出版年：2005
• 期刊代码：107_00404020
• 类别：ch
• 出版时间：April 4, 2005
• 卷：61
• 期：14
• 页码：3473-3481
• 文件大小：430 K

摘要

A robust synthetic method for 2-alkylamino-6-carboxy-5,7-diarylcyclopenteno[1,2-b]pyridines via acylamination at the alpha position of the functionalized pyridine system has been developed. The key step in this method was achieved by treatment of the corresponding pyridine N-oxides with 2.5equiv of imidoyl chlorides in the presence of triethylamine, thus producing the desired 2-acylaminopyridines in good yields (74–96%).