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Synthesis of novel 1-methyl-1H-pyridazino[3,4-b]indoles |
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| Authors: | Zsuzsanna Riedl Katrien Monsieurs Petra Dunkel Pál Tapolcsányi Sándor Boros Luc Pieters György Hajós |
| Institution: | a Chemical Research Center, Institute of Biomolecular Chemistry, Hungarian Academy of Sciences, H-1525 Budapest, PO Box 17, Hungary b Department of Chemistry, University of Antwerp, Groenenborgerlaan 171, B-2020 Antwerpen, Belgium c Department of Organic Chemistry, Semmelweis University, ‘Szentágothai János Tudásközpont’, H-1092 Budapest, H?gyes E. u. 7., Hungary d Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, B-2610 Antwerpen, Belgium |
| Abstract: | New synthetic pathways have been elaborated to 1-methyl-1H-pyridazino3,4-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. |
| Keywords: | Fused pyridazines Fused indoles Ring closure Suzuki coupling Antitrypanosomal activity |
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