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Oxazine derivatives R 0595 PTP-1B Inhibitors: Cyclopenta[d][1,2]-oxazine Derivatives. -Compound (VI), with nanomolar IC50 value, shows the highest activity and selectivity. It normalizes plasma glucose levels in mice but is only weakly active after oral dosing presumably due to low bioavailability (no yields given). -(CHOI*, J.-K.; et al.; Bioorg. Med.

We report a transition-metal-free deborylative cyclization approach to synthesize enantioenriched secondary and tertiary cyclopropylboronates using γ-phosphate-containing gem-diborylalkanes derived from chiral epoxides and gem-diborylalkanes. Our method enables the synthesis of a broad range of enantioenriched secondary and tertiary cyclopropylboronates in good yields with excellent stereospecificity. We demonstrate the versatility of our approach by performing a gram-scale reaction. We also show that the enantioenriched tertiary cyclopropylboronates can be transformed into a wide array of enantioenriched cyclopropane derivatives in a stereospecific boron-group transformation.