DG-041 is a small molecule antagonist of the EP3 receptor for
prostaglandin E2 that is in clinical development for treatment
of peripheral artery disease (PAD). Originally produced using
a six-step synthetic procedure, process optimization led to
development of a four-step sequence that is readily scalable.
The key step in the optimized sequence contains two sequential
Heck reactions, involving an intramolecular Heck cyclization
followed by an intermolecular Heck coupling, performed in one
pot to produce a highly substituted indole core.
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