An efficient method for the synthesis of bioactive heterocycles containing 1,2-benzothiazine 1,1-dioxide derivatives via Pd-catalyzed intramolecular Heck cyclization is reported. The method offers the regioselective synthesis of highly functionalized benzosultams in 80-85% yields. The structure of benzosultam derivatives is confirmed from single crystal X-ray diffraction.
A domino Sonogashira coupling and hydroamination reaction between o-iodo-N,N-dimethylaniline derivatives and propargyl sulfonamides are described. This protocol allows access to a variety of indole-2-methylsulfonamides in good to excellent yields. The structures of the synthesized compounds are confirmed by XRD studies.
Results and DiscussionThe required precursors of our present study, o-iodoaniline derivatives (20a-c) [15] and propargyl sulfonamide derivatives [a] S.
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