A flow process for Pd-catalyzed carbon fluorine bond formation is described. A microreactor using a packed-bed design allows for easy handling of large quantities of insoluble CsF with precise control over reaction times, efficient mixing, and the ability to safely handle elevated temperatures and pressures. A variety of aryl triflates, including heteroaryl ones, were converted to their corresp...

N(1)-Arylsulfonyl-substituted analogs of N,N-dimethyltryptamine bind at 5-HT(6) receptors. Replacement of the aryl moiety with similarly hydrophobic alkyl substituents results in decreased affinity, as does replacement of a benzenesulfonyl moiety with a benzyl group. Current findings indicate that an aryl (or substituted aryl) sulfonyl (rather than alkylsulfonyl or benzyl) moiety is optimal for...

Brønsted acidic ionic liquid triethylamine-bonded sulfonic acid {[Et3N-SO3H]Cl} efficiently catalyzes the one-pot multi-component condensation of 2-naphthol with arylaldehydes and dimedone (5,5-dimethylcyclohexane-1,3-dione) under solvent-free conditions to afford 12-aryl-8,9,10,12-tetrahydrobenzo[a]xanthen-11-ones in high yields and relatively short reaction times.

Based on the cooperative virulence index (c.f.) and LC(50) of fipronil, the interaction effect between short-term heat pretreatment and fipronil on 2(nd) instar larvae of diamondback moth (DBM), Plutella xylostella (Linnaeus), was assessed. The results suggested that pretreatment of the tested insects at 30 °C for 2, 4 and 8h could somewhat decrease the toxicity of fipronil at all set concentra...

In this work, some new heterocyclic systems 10-(aryl)-3-alkyl-6-methyl-6,8-dihydroimidazo[4′,5′:3,4]benzo[1,2-e][1, 4]diazepin-7(3H)-ones were obtained from the reaction of o-N-methylamino-ketone benzimidazoles with glycine in good yields. The structures compounds confirmed by elemental analyses, IR, mass, and NMR spectra. Also, their interactions studied vitro on recombinant benzodiazepine rec...

We describe here a tandem catalytic route to prepare imidazoles in a single operation from aryl iodides, imines and CO. The reaction involves a catalytic carbonylation of aryl halides with imines to form 1,3-dipoles, which undergo spontaneous 1,3-dipolar cycloaddition. Overall, this offers an alternative to coupling reactions to construct the (hetero)aryl-imidazole motif, where variation of the...

An equivalent amount of N-heteroaryl and aryl Grignard or lithium reagents, after mediation by an equivalent of titanate, was facilely coupled to furnish N-heteroaryl-aryl compounds under the catalysis of FeCl3/TMEDA at ambient temperature using oxygen as an oxidant. Most of the common N-heteroaryls were all good candidates, and thus provided a general, green and pratical protocol for the flexi...

Brønsted acidic ionic liquid triethylamine-bonded sulfonic acid {[Et3N-SO3H]Cl} efficiently catalyzes the one-pot multi-component condensation of 2-naphthol with arylaldehydes and dimedone (5,5-dimethylcyclohexane-1,3-dione) under solvent-free conditions to afford 12-aryl-8,9,10,12-tetrahydrobenzo[a]xanthen-11-ones in high yields and relatively short reaction times.