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Zhang, Haiming; Li, Beryl X; Wong, Brian; Stumpf, Andreas; Sowell, C. Gregory; Gosselin, Francis
Journal of organic chemistry, 04/2019, Letnik: 84, Številka: 8Journal Article
A practical convergent synthesis of PI3K inhibitor GDC-0908 (1) is described. The process features a dihydrobenzothienooxepine formation via palladium-catalyzed intramolecular direct C–H arylation and a Negishi coupling to construct the key C–C bonds. We further developed a general synthesis of dihydrobenzothienooxepines in good to excellent yields via palladium-catalyzed intramolecular direct C–H arylation, which tolerates both electronically and sterically diverse substituents on the phenyl ring.
