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Bicyclic amino acids as intermediates in the preparation of tricyclic amino acids and processes for their preparation
| Details |
Inventors: Urbach, Hansjorg; Henning, Rainer; Becker, Reinhard;
Assignee: Hoechst Aktiengesellschaft (DE)
Primary Examiner: Daus; Donald G.
Assistant Examiner: Shen; Cecilia
Attorney, Agent or Firm: Finnegan, Henderson, Farabow, Garrett & Dunner
The invention relates to new derivatives of tricyclic aminoacids, of the formula I ##STR1## in which n denotes 0 or 1, A denotes --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen, or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, or alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, or aralkyl or aroylalkyl, both of which can be substituted as defined above, or a monocyclic or bicyclic S--, O-- and/or N-heterocyclene radical, or a side chain of a naturally occurring aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and physiologically acceptable salts thereof, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation. |
|
DETAILED DESCRIPTION We claim: 1.
A compound of the formula III ##STR19## in which A denotes --CH.
dbd.
CH-- or --CH.
sub.
2 --CH.
sub.
2 --, the H atoms on C-2 and C-6 are in the cis-configuration relative to one another, the group --CO.
sub.
2 W on C-4 is orientated in the cis- or trans-position relative to the H atom on C-2 and the pyrrolidine ring is orientated in the exo- or endo-position relative to the bicyclic radical, and in which W denotes hydrogen; (C.
sub.
1 -C.
sub.
6)-alkyl or aralkyl with 7-9 carbon atoms.
2.
A compound of the formula III according to claim 1 wherein W denotes hydrogen, or a tert.
butyl or benzyl radical.
Description:
the invention relates to new derivatives of tricyclic aminoacids, of the formula I ##STR2## in which n denotes 0 or 1, A denotes --CH.
dbd.
CH-- or --CH.
sub.
2 --CH.
sub.
2 --, R denotes hydrogen, (C.
sub.
1 to C.
sub.
6)-alkyl or aralkyl with 7 to 9 carbon atoms, R.
sup.
1 denotes hydrogen, or (C.
sub.
1 to C.
sub.
6)-alkyl, which can be optionally substituted by amino, (C.
sub.
1 to C.
sub.
4)-acylamino, in particular (C.
sub.
1 to C.
sub.
4)-alkanoyl amino, or benzoylamino, or (C.
sub.
2 to C.
sub.
6)-alkenyl, (C.
sub.
5 to C.
sub.
9)-cycloalkyl, (C.
sub.
5 to C.
sub.
9)-cycloalkenyl, (C.
sub.
5 to C.
sub.
7)-cycloalkyl-(C.
sub.
1 to C.
sub.
4)-alkyl, (C.
sub.
6 to C.
sub.
12)-aryl or partially hydrogenated (C.
sub.
6 to C.
sub.
12)-aryl, each of which can be substituted by (C.
sub.
1 to C.
sub.
4)-alkyl, (C.
sub.
1 or C.
sub.
2)-alkoxy or halogen, or (C.
sub.
6 to C.
sub.
12)-aryl-(C.
sub.
1 to C.
sub.
4)-alkyl or (C.
sub.
7 to C.
sub.
13)-aroyl-(C.
sub.
1 to C.
sub.
4)-alkyl, both of which can be substituted in the aryl radical as defined above, or a monocyclic or bicyclic heterocyclene radical with 5 to 7 or 8 to 10 ring atoms, 1 or 2 ring atoms of which are sulfur or oxygen atoms and/or 1 to 4 ring atoms of which are nitrogen atoms, or a side chain of a naturally occurring aminoacid, which may be protected, R.
sup.
2 denotes hydrogen, (C.
sub.
1 to C.
sub.
6)-alkyl, (C.
sub.
2 to C.
sub.
6)-alkenyl or (C.
sub.
6 to C.
sub
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