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A synthetic methodology to access all possible stereoisomers of spectomycin A1 (SMA1) and A2 (SMA2) has been established through late‐stage diversification. The key reaction for the construction of all four diastereomers is an intramolecular cyclization based on the umpolung of π‐allyl palladium species with bis(pinacolato)diborane (B2(pin)2). Silyl group assisted direct benzylic oxidation of each...
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