Process and intermediate for certain bis-aza-bicyclic anxiolytic

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

1991-02-27

1993-02-09

Berch, Mark L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

544349, C07D227093, C07D47104

Patent

active

051854490

ABSTRACT:
(C.sub.1 -C.sub.3)Alkyl-4,6,7,8,9,9a-hexahydro-2H,3H-pyrido-[1,2-a]pyrazin-1-one-7- carboxylate esters, important precursors to certain bis-aza-bicyclic anxiolytics, can be prepared from di(C.sub.1 -C.sub.3)alkyl cis-piperidine-2,5-dicarboxylate starting material by a new process via a new class of intermediates, di(C.sub.1 -C.sub.3)alkyl cis-N-(2-(phthalimido)ethyl)piperidine-2,5-dicarboxylates. 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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