Compound <b>1</b> is a potent 5’-adenosine-monophosphate-activated protein kinase (AMPK) activator that was progressed to the clinic for the potential treatment of diabetic nephropathy. The development of the synthesis and the execution of the scale up campaigns to meet clinical and non-clinical studies will be described in addition to the synthesis of a major metabolite. Optimization of key steps included the formation of a methyl indole-3-carboxylate through acylation chemistry, palladium-mediated aryl-heteroaryl cross coupling, and an ester hydrolysis.

Development of the synthesis and scale-up of an AMPK activator clinical candidate

251st National Meeting (2016)

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