A "click and activate" approach in one-pot synthesis of a triazolyl-pyridazinone library
Wenyuan Qian1, David Winternheimer, Jennifer Allen
1Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States. wqian@amgen.com
Abstract:
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(I) catalyzed triazole formation which triggered subsequent nucleophilic substitution at the neighboring position to achieve three points of diversity.
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