Patent · US Expired

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

US5185449A · kind A · utility

3Cited by
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2Claims
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Assignee

Inventors

Key dates

Filing dateFeb 27, 1991
Grant dateFeb 9, 1993
Priority date
Expiry dateFeb 27, 2011

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D471/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.