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A neat and rapid procedure is reported for the synthesis of a variety of (2-aroyl-5-hydroxy-1,3,5- triaryl-4-piperidyl)(aryl)methanone (3a-3g) by the condensation of 2-((2-oxo-2- arylethyl)anilino)-1-aryl-1-ethanones 1 with different arylidene acetophenone 2 under microwave irradiation. Optically active 4-substitued piperidine derivatives have been recently synthesized from meso-3-substituted glutaric anhydride with (S)-methylbenzylamine. 7 An intramolecular anti- Markovnikov hydroamination of 1-(3-aminopropyl)vinylarenes resulted in the formation of 3- arylpiperidines. 8 A novel diastereoselective approach to 2,4-disubstituted piperidines involving the radical cyclization of 7-substituted 6-aza-8-bromooct-2-enoates has been recently reported. 9 Stereoselective syntheses of several differently functionalized piperidines have been recently reported. 10-14 Due to the importance of the piperdine chemistry, simple procedures for the formation of piperidines are highly desirable. In the present work, we describe an easy one pot synthesis of highly substituted piperidines from substituted N,N-diphenacylaniline 1.

A convenient one pot synthesis of highly substituted piperidines through a Michael addition-aldol cyclization sequence