3-Carbamoylmethyl-Indole-1-Carboxylic Acid Ethyl Ester (an ethoxycarbonyl derivative of indole-3-acetamide) is obtained by Friedel–Crafts type cyclocondensation γ-functionalized acetoacetamide in neat polyphosphoric acid.

N-glycosides of 6H-indolo[2,3-b]quinoxalines were prepared and structurally characterized. The synthesis relies on the cyclocondensation of isatine-N-glycosides with 1,2-diaminobenzenes. Some products exhibit weak cytotoxic activity against human ceratinocytes (HaCaT).

A straightforward and atom-economical method is described for the synthesis of 2,3-disubstituted indoles. Anilines and 1,2-diols are condensed under neat conditions with catalytic amounts of either [Cp*IrCl(2)](2)/MsOH or RuCl(3)·xH(2)O/phosphine (phosphine = PPh(3) or xantphos). The reaction does not require any stoichiometric additives and only produces water and dihydrogen as byproducts. Ani...

New series of thiazole derivatives were synthesized using 5-(aryldiazo)salicylaldehyde thiosemicarbazones 2a–i. Cyclocondensation 2a–i with chloroacetone afforded the corresponding 4-methylthiazole 3a–i. Moreover, cycloalkylation ethyl bromoacetate thiazolidin-4-one 4a–i. The antimicrobial activity new was evaluated.

An organocatalysed and chemoselective one-pot oxa-Michael-cyclocondensation reaction of N-BocNHOH to unsaturated α-ketoesters is reported which affords an original entry to enantioenriched 3-isoxazoline carboxylate derivatives as biorelevant heterocyclic frameworks.

The cyclocondensation of enones with aminoacetonitrile furnishes 3,4-dihydro-2H-pyrrole-2-carbonitriles which can be readily converted to 2,4-disubstituted pyrroles by microwave-induced dehydrocyanation. Alternatively, oxidation of the intermediates produces 3,5-disubstituted pyrrole-2-carbonitriles.

A concise synthesis of the marine alkaloids (-)-lepadins A-C from a phenylglycinol-derived tricyclic lactam is reported. Key steps from the stereochemical standpoint involve stereoselective cyclocondensation, double bond hydrogenation, oxazolidine opening, hydroboration-oxidation, and Horner-Wadsworth-Emmons reactions.

An N-heterocyclic carbene-catalyzed enantioselective [2+3] cyclocondensation of α-chloroaldehydes with azomethine imines was developed. The corresponding pyrazolidinones were obtained in good yields with moderate to good diastereoselectivities and excellent enantioselectivities.

The enantioselective N-heterocyclic carbene-catalyzed [4 + 2] cyclocondensation of 2-aryl carboxylic acids and enones was developed, affording the corresponding chiral δ-lactones in good yields with good diastereo- and high enantioselectivities.