Ruthenium-catalyzed Heck coupling of 3-arylidene-oxindoles with alkenes: a facile synthesis of 3-allylidene-2(3)-oxindoles.

A simple and efficient Ru(II)-catalyzed olefination of 3-(arylbenzylidene)indolin-2-ones with alkenes is described. This is an atom and step-economical strategy with a wide substrate scope, good functional group tolerance, and suitability for gram scale synthesis. A plausible mechanism is also proposed for this synthetic transformation involving the formation of a 5-membered ruthenacycle and insertion of the alkene followed by β-hydride elimination to deliver the desired product.

Palladium-Catalyzed Synthesis of Substituted Phenanthrenes via a C-H Annulation of 2-Biaryl Triflates with Alkynes.

A new palladium-catalyzed efficient method for the synthesis of substituted 9,10-phenanthrenes from 2-biaryl triflates with alkynes has been developed. This method provides a great opportunity to prepare various symmetrical and unsymmetrical phenanthrene derivatives in good yields. This reaction proceeds via C-OTf bond cleavage and alkyne insertion followed by C-H annulation.

Limited sampling strategies for therapeutic drug monitoring of anti-tuberculosis medications: A systematic review of their feasibility and clinical utility.

Therapeutic drug monitoring (TDM) is recommended for medications with high inter-individual variability, narrow therapeutic index drugs, possible drug-drug interactions, drug toxicity, and subtherapeutic concentrations, as well as to assess noncompliance. The area under the plasma concentration-time curve (AUC) is a significant pharmacokinetic parameter since it calculates the drug's total systematic exposure in the body. However, multiple blood samples from the patient are required to calculate the area under the curve, which is inconvenient for both the patient and the healthcare professional.

Rhodium-Catalyzed Annulations and Heck Coupling/Aza-Michael Addition for the Synthesis of Benzothiadiazinoisoquinoline 6,6-Dioxides and Benzothiadiazinoisoindole 5,5-Dioxides, Respectively.

A new and efficient protocol has been demonstrated for the synthesis of benzothiadiazinoisoquinoline 6,6-dioxides and benzothiadiazinoisoindole 5,5-dioxides in good to excellent yields. These compounds are formed through a sequential Rh(III)-catalyzed C-H cyclization of dihydrophenylbenzothiadiazine 1,1-dioxides with alkynes and oxidative Heck coupling/aza-Michael addition of dihydrophenylbenzothiadiazine 1,1-dioxides with acrylates, respectively.

Nickel-catalyzed [2 + 2 + 2] benzannulation of alkynes: a new route to the synthesis of highly substituted naphthalenes.

The Ni(II)-catalyzed aromatic homologation of various directing groups with alkynes to afford highly substituted naphthalene products C-X bond cleavage followed by alkyne insertion and C-H activation is described. This reaction proceeded with a wide range of directing groups such as pyrazoles, imidazopyridines, benzoimidazothiazoles, thiazoles and triazoles with alkynes to afford highly substituted naphthalenes in moderate to good yields. This transformation is promoted by a simple, straightforward combination of a Ni(II)-complex, Zn dust and a base.

Rh(III)-Catalyzed Oxidative C-2 Coupling of -Pyridinylindoles with Benzo[]thiophene 1,1-Dioxides via C-H Bond Activation.

An efficient Rh(III)-catalyzed cross-dehydrogenative coupling of -pyridinylindoles with benzo[]thiophene 1,1-dioxides has been developed through directing-group-assisted C-H activation. This transformation constructs a new C-C bond from two inert C-H bonds in a one-pot reaction. The present reaction is compatible with various functional groups with respect to indoles and benzothiophene[] 1,1-dioxides.

Catalyst-free 1,6-conjugate addition of indoles and 4-hydroxycoumarins to -quinone methides: synthesis of unsymmetrical triarylmethanes.

The catalyst-free 1,6-conjugate addition of indoles and 4-hydroxycoumarins to para-quinone methides is reported. This protocol allowed us to access a range of unsymmetrical triarylmethanes in good to excellent yields. The outlined procedure is operationally simple, efficient, atom and step economical.

Nickel-Catalyzed Cyclization Strategy for the Synthesis of Pyrroloquinolines, Indoloquinolines, and Indoloisoquinolines.

An inexpensive and benchtop stable Ni-catalyst/Zn system for the synthesis of pyrrolo/indoloquinolines and indolo[2,1-]isoquinolines is explored. This platform provides a one-pot entry for the preparation of various pyrrolo and indoloquinolines/isoquinolines, which involves successive C-C and C-N bond formation, respectively. In addition, we have also performed the preliminary photophysical studies for the synthesized compounds.

Rhodium(III)-Catalyzed Ortho Halogenations of N-Acylsulfoximines and Synthetic Applications toward Functionalized Sulfoximine Derivatives.

Rhodium(III)-catalyzed ortho brominations and iodinations of N-acylsulfoximines by C-H bond activations have been developed. Subsequent product functionalizations involving cross-coupling reactions provide alkynylated sulfoximine derivatives and benzothiazines with wide potential for further synthetic applications.

Hydroarylations of heterobicyclic alkenes through rhodium-catalyzed directed C-H functionalizations of S-aryl sulfoximines.

Rhodium-catalyzed directed CH-functionalizations have been used in hydroarylations of heterobicyclic alkenes with NH-sulfoximines. Unexpectedly, the bicyclic framework is retained, resulting in the formation of addition products being attractive intermediates for functionalized molecules that are difficult to prepare by other means.

One-pot synthesis of highly substituted polyheteroaromatic compounds by rhodium(III)-catalyzed multiple C-H activation and annulation.

A new method for the synthesis of highly substituted naphthyridine-based polyheteroaromatic compounds in high yields proceeds through rhodium(III)-catalyzed multiple C-H bond cleavage and C-C and C-N bond formation in a one-pot process. Such highly substituted polyheteroaromatic compounds have attracted much attention because of their unique π-conjugation, which make them suitable materials for organic semiconductors and luminescent materials. Furthermore, a possible mechanism, which involves multiple chelation-assisted ortho C-H activation, alkyne insertion, and reductive elimination, is proposed for this transformation.

Directed additions of 2-arylpyridines and related substrates to cyclic imines through rhodium-catalyzed C-H functionalization.

Rhodium-catalyzed C-H functionalizations have been used for ortho-directed additions of 2-arylpyridines and (hetero)aryl-substituted pyrimidines, isoquinolines, and benzo[h]quinolones to cyclic imines. The resulting amino-functionalized products are formed in good to high yields.

Iron-catalyzed hetero-cross-dehydrogenative coupling reactions of sulfoximines with diarylmethanes: a new route to N-alkylated sulfoximines.

An efficient iron-catalyzed C-N bond formation by hetero-cross-dehydrogenative coupling (CDC) between sulfoximines and diarylmethanes is described. The reaction shows good functional group tolerance and provides N-alkylated sulfoximines in moderate to good yields.

Rhodium(III)-catalyzed selective ortho-olefinations of N-acyl and N-aroyl sulfoximines by C-H bond activation.

Two new rhodium-catalyzed oxidative couplings between sulfoximine derivatives and alkenes by regioselective CH activation, affording ortho-olefinated (Heck-type) products, are reported. A synthetic application of the ortho-alkenylated products into the corresponding cyclic derivatives has been demonstrated, and a mechanistic rational for the rhodium catalysis is presented.

Rh(III) -catalyzed C-H activation: a versatile route towards various polycyclic pyridinium salts.

An efficient and convenient method for the synthesis of highly substituted polycyclic pyridinium salts from the reaction of various 2-aryl-pyridines and 2-aryl-sp(2) -nitrogen-atom-containing heterocycles with alkynes through rhodium(III)-catalyzed CH activation and annulation under an O2 atmosphere is described. A possible mechanism that involves the chelation-assisted CH activation of the 2-aryl-pyridine substrate, insertion of the alkyne, and reductive elimination is proposed. This mechanism was supported by the isolation of a five-membered rhodacycle (I').

Rhodium-catalyzed oxidative annulation of sulfoximines and alkynes as an approach to 1,2-benzothiazines.

Revitalization by oxygen: A rhodium(III)-catalyzed oxidative CH/NH activation/annulation sequence provided access to a variety of substituted 1,2-benzothiazine derivatives from readily available NH-sulfoximines and alkynes (see scheme; Cp*=C5 Me5 ). The oxidation system consisted of molecular oxygen in combination with a catalytic amount of Fe(OAc)2 .

Synthesis of Phenanthridinones from N-methoxybenzamides and aryltriethoxysilanes through Rh(III)-catalyzed C-H and N-H bond activation.

An efficient method for the one-pot synthesis of substituted phenanthridinone derivatives from N-methoxybenzamides and aryltriethoxysilanes through rhodium-catalyzed dual C-H bond activation and annulation reactions is described. A double-cycle mechanism is proposed to account for this catalytic reaction. In addition, isotope-labeling studies were performed to understand the intimate mechanism of the reaction.

Ru(II)-catalyzed amidation of 2-arylpyridines with isocyanates via C-H activation.

An efficient Ru(II)-catalyzed amidation of 2-arylpyridines with isocyanates via C-H bond activation is described.

Ru(II)-catalyzed C-H bond activation for the synthesis of substituted isoquinolinium salts from benzaldehydes, amines, and alkynes.

An efficient method for the synthesis of substituted isoquinolinium salts from benzaldehydes, amines, and alkynes via ruthenium-catalyzed C-H bond activation and annulation in one pot is described.

Synthesis of isochromenones and oxepines via Pd-catalyzed cascade cyclization of alkynes and benzynes involving C-H activation.

A new method for the synthesis of various isochromen-6-ones and phenanthro[1,10-bc]oxepines via a palladium-catalyzed cascade carbocyclization of 2-iodobenzyl-3-phenylpropiolates and 1-iodo-2-(2-(phenylethynyl)benzyloxy)benzenes with arynes is described. The reactions involve interesting biscarbocyclization of alkynes and benzynes and C-H bond activation.

Nickel-catalyzed cyclization of ortho-iodoketoximes and ortho-iodoketimines with alkynes: synthesis of highly substituted isoquinolines and isoquinolinium salts.

A convenient method for the synthesis of highly substituted isoquinolines and isoquinolinium salts by the nickel-catalyzed cyclization of ortho-haloketoximes and -ketimines, respectively, with alkynes is described. The reaction of ortho-haloketoximes and various alkynes in the presence of [Ni(PPh(3))(2)Br(2)] and zinc powder in a mixture of acetonitrile and tetrahydrofuran at 80 °C for 15 hours gave 1,3,4-trisubstituted isoquinoline products in moderate to excellent yields and high regioselectivity. The corresponding isoquinoline N-oxide was found to be the intermediate in the cyclization reaction pathway.

Synthesis of biarylketones and phthalides from organoboronic acids and aldehydes catalyzed by cobalt complexes.

A cobalt-catalyzed addition of aryl- and alkenylboronic acids to aldehydes and phthalaldehyde to give the corresponding biarylketones and 3-aryl phthalides in good to excellent yields in one pot is described.