2-Aryl-6-cyano-7-methyl-5-indolizinones were successfully converted into 2-aryl-5-chloro-6-cyano-7-methylindolizines. The obtained 5-chloroindolizines readily underwent nucleophilic substitution at position 5 leading in high yields to novel 5-functionalised indolizines.

2-(Alkyl(aryl)amino)thiazol-4(5H)-ones can regioselectively be prepared from monoalkyl(aryl)thioureas and maleimides. In solution, the former heterocycles exist in a tautomeric equilibrium with 2-(alkyl(aryl)imino)thiazolidin-4-ones and the substituent on the exocyclic nitrogen atom governs the ratio of these tautomers. Isomers with the alkyl group in the endocyclic position can be obtained fro...

Chart 1) were reported to inhibit colon and lung tumors in a patent literature. Subsequently, we found that 3-aryl b-carbolin-1-ones (2) inhibit the proliferation of HeLa cells with IC50 values in the low micromolar range and that the aromatic substitution on C3 in 2 proved to be essential for their biological activity. To broaden the scope of previous studies, aryl-substituted 2-pyridone-conta...

A bidentate nitrogen-donor ligand with an appended phenol group, C5H4NCH[double bond, length as m-dash]N-2-C6H4OH, H(L1) was treated with a palladium cycloneophyl complex [Pd(CH2CMe2C6H4)(COD)], with both Pd-aryl and Pd-alkyl bonds, to give a Pd-alkyl complex, [Pd(CH2CMe2C6H5)(κ3-N,N',O-OC6H4N[double bond, length as m-dash]CH(2-C5H4N))], 1. The cleavage of the Pd-aryl bond and the deprotonation...

P,N,N-Pincer nickel complexes [Ni(Cl){N(2-R2PC6H4)(2'-Me2NC6H4)}] (R = Ph, 3a; R = Pr(i), 3b; R = Cy, 3c) were synthesized and their catalysis toward the Kumada or Negishi cross-coupling reaction of aryl fluorides and chlorides was evaluated. Complex 3a effectively catalyzes the cross-coupling of (hetero)aryl fluorides with aryl Grignard reagents at room temperature. Complex 3a also catalyzes t...

The total syntheses of the Lythracea alkaloids (+)-vertine and (+)-lythrine are described. Enantioenriched pelletierine is used as a chiral building block and engaged into a two step pelletierine condensation leading to two quinolizidin-2-one diastereomers in a 8 : 1 ratio. The major product is used in the synthesis of (+)-vertine via aryl-aryl coupling and ring closing metathesis to provide a ...

1-C and 2-C-branched carbohydrates are present as substructures in a number of biologically important compounds. Although the synthesis of such carbohydrate derivatives is extensively studied, the synthesis of 1,2-cis-2-C-branched C-, S-, and N-glycosides is less explored. In this article a synthetic strategy for the synthesis of 1,2-cis-2-C-branched-aryl-C-glucosides is reported via a hydrogen...

The first palladium-catalyzed dearomative cyclization via a modified Catellani-type C-H functionalization has been realized. The new strategy led to a series of spiroindolenine derivatives bearing an all-carbon quaternary spirocenter from simple aryl halides and substituted indoles.

An efficient method has been developed for the catalysis of condensation of 1,2-phenylenediamines and 2-aminothiophenoles with different aldehydes into their corresponding 2-aryl-1H-benzimidazoles and 2-aryl-1H-benzothiazoles under mild condition. In this method, trans-3,5-dihydroperoxy-3,5-dimethyl-1,2-dioxolane (DHPDMDO)/HOAc/KI system was used as a novel and effective oxidant in water at roo...