An efficient and mild one-pot convergent synthesis protocol has been developed for benzo[b]oxazolo[3,4-d][1,4]oxazin-1-one derivatives through the Mitsunobu reaction and sequential cyclization.

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6,6-Dimethyl-3-azabicyclo [3.1.0]hexane (6,6-DMABH) is a fundamental building block in numerous antiviral drugs, including boceprevir and pf-07321332. To enable more efficient synthesis of 6,6-DMABH, we developed an innovative approach that utilizes the intramolecular cyclopropanation of alpha-diazoacetates via Ru (II) catalysis and Gabriel synthesis. Our method enabled the synthesis of 6,6-DMABH from 3-methyl-2-butenol in seven distinct steps, yielding a total of 28%.