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Title: Generation of 3-piperidine(methan)amines and cyclic 3-piperidinemethanamines as potential Substance P antagonists
Authors: Knoops, Nele ×
Deroover, G
Zhang, JD
Compernolle, Frans
Hoornaert, Georges #
Issue Date: Jan-1997
Publisher: Pergamon-elsevier science ltd
Series Title: Tetrahedron vol:53 issue:37 pages:12699-12716
Abstract: A general method is described for the synthesis of 3-piperidine(methan)amines and their cyclic analogues. The 3,5-dichloro-2H-1,4-oxazin-2-ones 6 and 3-aryl substituted analogues are reacted with acetylenic dienophiles yielding pyridines. Further catalytic hydrogenation and functional group transformation (1) or substitution (2-3) with ring closure reactions (4) followed by hydrogenation provided the 2,3,5-cis substituted piperidines 1-3 and a cis substituted [3,4-c]pyrrolopiperidine 4. These compounds have recently raised great interest due to their Substance P antagonist profiles. (C) 1997 Elsevier Science Ltd.
URI: 
ISSN: 0040-4020
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Chemistry - miscellaneous
Molecular Design and Synthesis
× corresponding author
# (joint) last author

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