4.8 Article

A Click and Activate Approach in One-Pot Synthesis of a Triazolyl-Pyridazinone Library

Journal

ORGANIC LETTERS
Volume 13, Issue 7, Pages 1682-1685

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol200183b

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Funding

  1. Amgen CRD

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A click and activate strategy was designed and executed in a four-component, stepwise condensation that led to a trisubstituted triazolyl-pyridazinone library. This one-pot process included regioselective azide substitution at 2-substituted-4,5-dichloropyridazinones, followed by a Cu(l) catalyzed triazole formation which triggered subsequent nucleophilic substitution at the neighboring position to achieve three points of diversity.

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