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[摘要]：Enantiomerically enriched forms of a sulfoximine-based myristic acid analogue are prepared using either an asymmetric desymmetrization with a chiral base, or an enantioselective oxidation procedure as key steps. Additionally, a variety of 2-oxa-2-alkyl 3,4-dihydro 2,1-benzothiazines are synthesized via intramolecular metal-catalyzed N-arylation of appropriately functionalized sulfoximines with tethered 2-bromoaryl substituents. In turn, the sulfoximines are prepared by lithiation-alkylation sequences including enantioselective deprotonation steps or the use of an optically active sulfoxide. Using this methodology, the range of accessible 3,4-dihydro 2,1-benzothiazine derivatives is expanded. |
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