The present review provides a comprehensive summary of the catalytic and catalyst-free diboration of alkynes.

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

An efficient Rh­(III)-catalyzed C–H alkenylation/directing group migration cascade between indoles and alkynes for the assembly of tetrasubstituted alkenes is reported. The carbamoyl directing group migrates to the carbon of the alkene moiety of the products through rare Rh-catalyzed C–N bond cleavage after the C–H alkenylation step and thus acts as an internal amidation reagent. This protocol shows broad substrate scope, excellent regio/stereoselectivity, and good to excellent yields.

No abstract

Palladium-catalyzed ortho-C–H olefination of phenylalanine and phenylethylamine derivatives assisted by a removable picolinamide group has been achieved.

The present study describes an AuPPh3Cl/AgSbF6-catalyzed cascade reaction between amine nucleophiles and alkynoic acids in water. This process proceeds in high step economy with water as the sole coproduct, and leads to the generation of two rings, together with the formation of three new bonds in a single operation. This green cascade process exhibits valuable features such as low catalyst loading, good to excellent yields, high efficiency in bond formation, excellent selectivity, great tolerance of functional groups, and extraordinarily broad substrate scope. In addition, this is the first example of the generation of an indole/thiophene/pyrrole/pyridine/naphthalene/benzene-fused N-heterocycle library through gold catalysis in water from readily available materials. Notably, the discovery of antibacterial molecules from this library demonstrates its high quality and potential for the identification of active pharmaceutical ingredients.