Anew SO 2 surrogate is reported that is cheap,benchstable,a nd can be accessed in just two steps from bulk chemicals.E ssentially complete SO 2 release is achieved in 5minutes.Eight established sulfonylation reactions proceeded smoothly by ex situ formation of SO 2 by utilizing at wochamber system in combination with the SO 2 surrogate. Furthermore,w er eport the first direct aminosulfonylation between aryl iodides and amines.B road functional group tolerance is demonstrated, and the method is applicable to pharmaceutically relevant substrates,i ncluding heterocyclic substrates.
Herein we report the additive-controlled divergent synthesis of tetrasubstituted 1,3-enynes and alkynylated 3Hpyrrolo[1,2-a]indol-3-ones through rhodium-catalyzed C-H alkenylation/DG migration and [3+2] annulation, respectively. This protocol features rare directing group migration in 1,3-diyne-involved C-H activation, excellent regio-and stereoselectivity, excellent monofunctionalization over difunctionalization, broad substrate scope, moderate to high yields, good functional group compatibility and mild redox-neutral conditions.
1,3-unsubstituted 2-(1H-indol-2-yl)ethanamines were employed for the first time to react with alkynoic acids (AAs) to achieve gold-catalyzed highly selective cascade reactions to furnish novel indole-fused skeletons. Furthermore, with this powerful gold catalytic system, a library of indole/pyrrole/thiophene/benzene/naphthalene/ pyridine-based nitrogen-containing heterocyclic compounds (NCHCs) with scaffold diversity and molecular complexity was constructed rapidly using various amine nucleophiles (ANs) and diverse AAs as the building blocks. This general protocol features excellent selectivity, extraordinarily broad substrate scope, readily available inputs, good to high yields, high bond-forming efficiency, and step economy, thus providing a facile and efficient access to a variety of valuable nitrogen-containing heterocycles. LRMS (ESI) m/z: 218 [M + H] + ; HRMS (ESI) m/z calculated for C 12 H 11 NO 3 + H + 218.0812, found: 218.0809. 2 3 4 5 6 7 8
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