Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1982-05-17
1984-05-29
Jiles, Henry R.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C07D47104
Patent
active
044516550
ABSTRACT:
A novel process for preparing various 2-substituted-5-aryl-1,2,3,4-tetrahydro-.gamma.-carboline derivatives is provided, which involves (1) quaternizing a corresponding 5-aryl-.gamma.-carboline compound with an appropriate aralkyl halide in the presence of sodium iodide, followed by (2) reduction of the corresponding quaternary carbolinium iodide salt intermediate with an alkali metal hydride to yield the desired final product. The latter compounds are known to be useful as tranquilizing agents, with 2-[4-(p-fluorophenyl)-4-hydroxybutyl]-5-(p-fluorophenyl)-8-fluoro-1,2,3,4- tetrahydro-.gamma.-carboline representing a preferred final product. The aforesaid carbolinium salt intermediates as well as the corresponding 5-aryl-.gamma.-carboline starting materials are all novel compounds.
REFERENCES:
patent: 2819997 (1956-01-01), McLamore
patent: 4001263 (1974-01-01), Plattner et al.
Dalton et al., Australian J. of Chem., (1969), vol. 22, pp. 185-195.
C. A. Harbert et al., in the Journal of Medicinal Chemistry, vol. 23, p. 635, (1980).
Dentz Bernard
Jiles Henry R.
Knuth Charles J.
Pfizer Inc.
Richardson Peter C.
LandOfFree
Process for preparing carboline derivatives and compounds used i does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Process for preparing carboline derivatives and compounds used i, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for preparing carboline derivatives and compounds used i will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1398888