Joanna Wlochal, Andrew Bailey
Dec 2, 2015
Citations
0
Influential Citations
6
Citations
Journal
Tetrahedron Letters
Abstract
Substituted pyridazine-3,6-diamines are attractive but poorly precedented scaffolds in medicinal chemistry and are challenging targets in terms of synthetic tractability. In the following communication we report the use of a Buchwald protocol for the facile synthesis of 4-aryl and alkyl substituted, N6-alkylated pyridazine-3,6-diamines. This approach utilises the unreactive nature of the pyridazine 3-amino group, negating the need for an additional protecting group in the transformation. The relevant precursors were prepared by selective Suzuki or Negishi transformations using commercially available 4-bromo-6-chloro-3-pyridazinamine.