Derivatives of bicyclic amino acids, process for t

专利名称：Derivatives of bicyclic amino acids, process

for their preparation, agents containingthem and their use, as well as bicyclic aminoacids as intermediates, and process forpreparing them

发明人：Urbach, Hansjörg, Dr.,Henning, Rainer,

Dr.,Teetz, Volker, Dr.,Geiger, Rolf, Prof.Dr.,Becker, Reinhard, Dr.,Gaul, Holger

申请号：EP82112007申请日：19821224公开号：EP00841A3公开日：19831012

摘要：1. Claims for the Contracting states ; BE, CH, DE, FR, GB, IT, Li, Lu, NL, SE Acompound of the formula I see diagramm : EP00841,P21,F7 in which the hydrogenatoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative toone another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen,(C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y andZ together denote oxygen and X denotes phenyl, and its physiologically acceptable salts.1. Claims for the Contracting state : Austria A process for the preparation of thecompounds of the formula I see diagramm : EP00841,P24,F4 in which the hydrogenatoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative toone another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen,(C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and

Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts,which a) comprises reacting a compound of the formula II see diagramm :

EP00841,P24,F6 wherein R1 , R2 , X, Y and Z have the meanings as in formula I, with acompound of the formula III see diagramm : EP00841,P25,F1 in which the H atoms onthe C atoms 3a and (6+n)a have the trans configuration relative to one another andwherein n denotes 0, 1 or 2 and W denotes a radical which can be cleaved off byhydrogenolysis or by acid, and subsequently splitting off the radical W and, if

appropriate, the radical R2 to form the free carboxyl groups, or b) for the preparation ofcompounds of the formula I, in which Y and Z together denote oxygen, comprises b1 )reacting a compound of the formula IV see diagramm : EP00841,P25,F3 in which the Hatoms on the C atoms 3a and (6+n)a have the trans configuration relative to one anotherand wherein n and R1 have the meanings as in formula I and W has the meaning as informula III, with a compound of the formula V, R2 O2 C-CH = CH-CO-X wherein R2 and Xhave the meanings as in formula I, and subsequently splitting off the radical W and, ifappropriate, also the radical R2 to form the free carboxyl groups, or, b2 ) reacting acompound of the formula IV mentioned under b1 ) with a compound of the generalformula VI, wherein R2 has the meaning as in formula I, and with a compound of thegeneral formula VII OHC-CO2 R2 X-CO-CH3 wherein X has the meaning as in formula I,subsequently splitting off the radical W and, if appropriate, the radical R2 to form thefree carboxyl group, or c) for the preparation of compounds of the formula I, in which Yand Z each denote hydrogen, comprises c1 ) reacting a compound of the formula IVmentioned under b1 ) with a compound of the formula VIII see diagramm :

EP00841,P25,F2 wherein R2 and X have the meanings as in formula I, reducing theSchiff's bases obtained and subsequently splitting off the radical W and, if appropriate,the radical R2 to form the free carboxyl groups, or c2 ) catalytically reducing a compoundof the formula I in which Y and Z together denote oxygen, with hydrogen, or d) for thepreparation of compounds of the formula I, in which Y denotes hydroxyl and Z denoteshydrogen, comprises reducing a compound of the formula I, in which Y and Z together

denote oxygen, catalytically with hydrogen or with a reducing agent, such as sodiumborohydride, and, if appropriate, converting the compounds obtained according to (a)-(d)into their physiologically acceptable salts.

申请人：HOECHST AKTIENGESELLSCHAFT

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