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An efficient synthesis of a pyrrolo-azepine scaffold for the parallel preparation of an array of (oxo-pyrrolo-azepinyl)-acetamides is described. The Stetter cyclisation of 1,3-cyclohexanedione with ethyl bromopyruvate was the key reaction in the assembly of a tetrahydrobenzofuran substrate which was submitted to a rapid transformation into a tetrahydroindole by microwave-assisted cyclocondensation in the presence of glycine. The carbonyl group was then stereoselectively transformed into the corresponding (Z)-oxime which

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Using a commercially available device for controlled introduction of hydrogen in a vial for reactions under microwave dielectric heating, we developed a protocol for the transformation of substituted pyridines into the corresponding piperidines. Complete reduction occurred in 40 minutes, or even less, on substrates that require 24-48 hours to be reduced under standard conditions. Moreover, the reduction proved to be as stereoselective as the corresponding reaction carried out at room temperature.

Multi-membered N-heterocycles R 0690Scaffold Preparation and Parallel Synthesis of Arrays of 5,6,7,8-Tetrahydropyrrolo-azepinones in the Solution Phase. -A novel and optimized procedure for the preparation of scaffold (VII) in multigram scale is reported. Diversification in 1-and 5-position of the ring is achieved in solution-phase combinatorial synthesis affording an array of 52 new products. -(PIRAS, L.; GENESIO, E.; GHIRON, C.; TADDEI*, M.; Eur.