An Intra/Intermolecular Suzuki Sequence to Benzopyridyloxepines Containing Geometrically Pure Exocyclic Tetrasubstituted Alkenes.

[摘要]：A route to enable the prepn. of 5-benzylidenyl-benzopyridyloxepine analogs, e.g., I (R1 = Me, Et, i-Pr; R2 = H, F, MeO), was developed to continue our research in the field of nuclear hormone receptor modulators. The key steps are: 1. a syn-stereoselective diboration of a tethered aryl alkyne; 2. an intramol. Suzuki cross-coupling reaction, which forms in a stereo- and regiocontrolled fashion, the 5-exoalkylidenyl 7-membered ring imbedded within the core of the scaffold and; 3. an intermol. Suzuki to furnish the final tetra-substituted olefinic benzopyridyloxepines.

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