Abstract

We have devised an asymmetric route to the tricyclic core 10 of BMS-986251. The six-step synthesis utilizes readily available starting materials, involves the one-step installation of the perfluoro isopropyl moiety through a radical mechanism, and leverages a novel diastereoselective annulation to build the pyrrolidine ring. Overall, 10 was obtained in 49% yield as a single stereoisomer in 6 steps and 3 isolations using this new route.

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