Discovery and Synthesis of a Direct Activator of AMP-Kinase PF-06409577 against Diabetic Nephropathy

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Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. PF-06409577 has been discovered as an indole acid with excellent balance of properties and has now been advanced to first-in-human trials for the treatment of diabetic nephropathy. Key indazoles in the synthesis were prepared by Suzuki coupling to some commercially available 5-bromoindazoles (scheme).

SiliaMetS Thiol was used to remove remaining Pd after only 30 min of stirring.

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