A robust synthetic route—featuring a convergent Suzuki–Miyaura coupling, an enantioselective reduction, and a late‑stage amide bond formation—enables kilogram‑scale production under GMP conditions with an overall yield of 42 %. Pre‑clinical studies demonstrated complete tumor regression in xenograft models of triple‑negative breast cancer (TNBC) and substantial disease‑modifying effects in a mouse model of multiple sclerosis (EAE).
Overall isolated yield from starting materials: over eight steps. The route is amenable to scale‑up, with each step validated on 100 g–1 kg scale. Key process considerations include: MEYD-873
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