Bicyclic aminoacids as intermediates

Details Bicyclic aminoacids as intermediates Bicyclic aminoacids as intermediates

1984-11-21

1991-04-16

Hollrah, Glennon H.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546158, 548515, C07D20912, C07D20952

Patent

active

050084003

ABSTRACT:
Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0,1 or 2, R.sub.1 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl which can optionally by substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 -C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 -C.sub.2)-alkyl, (C.sub.2 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C.sub.1 - C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, hydroxyl, halogen, nitro, amino, (C.sub.1 -C.sub.4)-alkylamino, di-(C.sub.1 -C.sub.4)-alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process for the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.

REFERENCES:
patent: 4344449 (1982-11-01), Hoefle et al.
patent: 4350704 (1982-09-01), Hoefle et al.
patent: 4404206 (1983-09-01), Vincent et al.
patent: 4468396 (1984-08-01), Magatti
patent: 4490386 (1984-12-01), Seamans et al.
patent: 4559340 (1985-12-01), Neustadt et al.

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