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Optically active bicyclic imino-alpha-carboxylic esters
| Details |
Inventors: Geiger, Rolf; Teetz, Volker; Langner, Dietrich; Urbach, Hansjorg; Henning, Rainer;
Assignee: Hoechst Aktiengesellschaft (DE)
Primary Examiner: Springer; David B.
Assistant Examiner:
Attorney, Agent or Firm: Finnegan, Henderson, Farabow, Garrett & Dunner
The invention relates to a process for resolving racemic mixtures of bicyclic imino-.alpha.-carboxylic esters into the components by crystallization of diastereomeric salts, which comprises preparing the salts of the racemic esters with optically active N-acylated R- or S-amino carboxylic acids which contain a phenyl nucleus, recrystallizing them from an organic solvent, decomposing the precipitated, optically homogeneous diastereomeric salts in a manner known per se, and isolating the enantiomers and, where appropriate, converting the latter into the free acids by hydrolysis in a manner known per se. The invention also relates to optically pure compounds of the formula ##STR1## and to diastereomeric salts of these compounds, in which two of the radicals A, B.sup.1, B.sup.2 and C form a carbon chain and the others denote hydrogen, and R is an esterifying group. |
|
DETAILED DESCRIPTION We claim: 1.
A compound of the formulae Ia or Ib essentially free of its racemate, and salts of said compound, ##STR15## in which the two bridgehead hydrogen atoms have the cis configuration, the COOR group is oriented endo with respect to the bicyclic ring system, the carbon atom .
alpha.
to the COOR group has the R or S configuration, (a) A and B.
sup.
1 denote hydrogen, and B.
sup.
2 and C together form a chain of the formula --(CH.
sub.
2).
sub.
n --, with n being 3, 4, 5, 6 or a chain of the formula --(CH.
sub.
2).
sub.
p --CH.
dbd.
CH(CH.
sub.
2).
sub.
q --, with (p+q) being 1, 2, 3 or 4, or (b) C and B.
sup.
2 denote hydrogen and A and B.
sup.
1 together form one of the chains defined above under (a), and (c) R represents alkyl having 1 to 6 carbon atoms, cycloalkyl having 4 to 8 carbon atoms or aralkyl having 7 to 13 carbon atoms which can optionally be substituted by NO.
sub.
2.
2.
A compound of the formulae Ia or Ib, and its salts, ##STR16## in which the two bridgehead hydrogen atoms have the cis configuration, the COOR group is oriented endo with respect to the bicyclic ring system, the carbon atom .
alpha.
to the COOR group has the R or S configuration, and R denotes hydrogen or represents alkyl having 1 to 6 carbon atoms, cycloalkyl having 4 to 8 carbon atoms or aralkyl having 7 to 13 carbon atoms which can optionally be substituted by NO.
sub.
2, (a) A and B.
sup.
1 denote hydrogen, and B.
sup.
2 and C together form a chain of the formula --(CH.
sub.
2).
sub.
n --, with n being 3, 4, 5 or 6, or a chain of the formula --(CH.
sub.
2).
sub.
p --CH.
dbd.
CH--(CH.
sub.
2).
sub.
q --, with (p+q) being 1, 2, 3 or 4, or (b) C and B.
sup.
2 denote hydrogen, and A and B.
sup.
1 together form one of the chains defined above under (a) with n being 3, 5, or 6 and (p+q) being 1, 2, 3, or 4.
3.
A compound as claimed in claim 1, wherein the carbon atom .
alpha.
to the COOR group has the S configuration.
4.
A compound as claimed in claim 2, wherein the carbon atom .
alpha.
to the COOR group has the S configuration.
Description:
The resolution of racemates of aminoacids via crystallization of diastereomeric salts is a widely used process (Review: Boyle, Quart
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Vasodialators 
