Process and intermediate for certain bis-aza-bicyclic...

Details Process and intermediate for certain bis-aza-bicyclic... Process and intermediate for certain bis-aza-bicyclic...

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2101433

C1-C3)Alkyl-4, 6, 7, 8, 9, 9a-hexahydro-2H, 3H-pyrido-[1,2-a]pyrazin-1-one-7-carboxylate esters (111), important precursors to certain bis-aza-bicyclic anxiolytics, can be prepared from di(C1-C3)alkyl cis-piperidine-2,5-dicarboxylate starting material by a new process via a new class of intermediates di(C1-C3)alkyl cis-N-(2-(phthalimido)ethyl)piperidine-2,5-dicar-boxylates (11). In the process, the starting material is reacted with either 2-(phthalimido)ethyl triflate or 2-(phthalimido)-acetaldehyde to form the new intermediate, which can then be cyclized to the aforementioned precursor.

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