Facile synthesis of 4-aryl and alkyl substituted, N6-alkylated pyridazine-3,6-diamines
摘要：
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.
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关键词：
Substituted pyridazine-3,6-diamines 3,6-Diaminopyridazines Brettphos precatalyst Buchwald protocol
DOI：
10.1016/j.tetlet.2015.10.075
被引量：
年份：
2015
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