An efficient protocol for facile construction of 3,4-dihydro-10-iodo-3-iodomethylene-[1,4]oxazino[4,3-a]indol-1-ones has been developed by using a regio-and stereoselective iodolactonization reaction. Subsequent palladium cross-coupling reactions of 3,4-dihydro-10-iodo-3-iodomethylene-[1,4]-oxazino[4,3-a]indol-1-ones readily afforded functionalized oxazinoindolones.
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