Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1978-05-12
1979-11-20
Rotman, Alan L.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
546348, 546350, 546344, C07D21304, C07D21330
Patent
active
041751973
ABSTRACT:
Novel 1,3,4-trisubstituted-4-arylpiperidines are prepared by alkylating a 2,3-disubstituted-3-arylpyrroline to afford a 1,2,3-trisubstituted-3-aryl-1-pyrrolinium salt, reacting the salt with diazomethane to provide a 1,2,3-trisubstituted-3-aryl-1,2-methylene-pyrrolidinium salt, heating the pyrrolidinium salt to effect a ring expansion to the corresponding 1,3,4-trisubstituted-4-aryl-1,4,5,6-tetrahydropyridinium salt, neutralizing the salt and reducing the tetrahydropyridine to provide a 1,3,4-trisubstituted-4-arylpiperidine. The piperidines so formed are useful as pharmacological agents and as intermediates in the preparation of other piperidines of the invention. The compounds provided herein are especially useful as narcotic agonists analgesics and as narcotic antagonists.
REFERENCES:
patent: 2748140 (1956-05-01), Schmidle et al.
patent: 3125488 (1964-03-01), Biel
patent: 3716543 (1973-02-01), Hall
patent: 3847930 (1974-11-01), Randell et al.
patent: 4001414 (1977-01-01), Granados et al.
patent: 4028371 (1977-06-01), Granados et al.
Ashbrook Charles W.
Eli Lilly and Company
Rotman Alan L.
Smith Everet F.
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