Synthesis of novel 1-methyl-1H-pyridazino[3,4-b]indoles

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• 作者：Zsuzsanna Riedl ; Katrien Monsieurs ; Gá ; bor Krajsovszky ; Petra Dunkel ; Bert U.W. Maes ; Pá ; l Tapolcsá ; nyi ; Orsolya Egyed ; Sá ; ndor Boros ; Pé ; ter Má ; tyus ; Luc Pieters et al.
• 关键词：Fused pyridazines ; Fused indoles ; Ring closure ; Suzuki coupling ; Antitrypanosomal activity
• 刊名：Tetrahedron
• 出版年：2006
• 期刊代码：107_00404020
• 类别：ch
• 出版时间：2 January 2006
• 卷：62
• 期：1
• 页码：121-129
• 文件大小：273 K

摘要

New synthetic pathways have been elaborated to 1-methyl-1H-pyridazino[3,4-b]indoles starting from halopyridazin-3(2H)-ones. Suzuki cross-coupling reaction of chloro, iodo, dichloro, and dibromo substituted pyridazin-3(2H)-ones with 2-pivaloylaminophenylboronic acid followed by hydrolysis of the amide and subsequent ring closure via condensation gave fused indoles. Some of these compounds showed biological activity as antitrypanosomal agents.