Claims
- 1. A process for the preparation of a racemic or optically active compound of the formula (I) ##STR12## wherein R means hydrogen or a straight or branched chain C.sub.1-6 alkoxy group;
- R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group;
- R.sup.2 represents hydrogen or a straight or branched chain C.sub.1-6 alkyl group;
- R.sup.3 means hydrogen; a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group;
- R.sup.4 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group; and R.sup.3 and R.sup.4 together with the nitrogen atom, to which they are attached form a 4 to 8-membered cyclic group of formula ##STR13## optionally substituted by one or two straight or branched chain C.sub.1-4 alkoxy and/or one or two straight or branched chain C.sub.1-4 alkyl group(s), where optionally an oxygen or sulfur atom or an N-R.sup.5 group may be substituted for a ring carbon atom, where R.sup.5 means hydrogen or a straight or branched chain C.sub.1-6 aliphatic alkyl group, the 4- to 8-membered cycle optionally being condensed with a benzene ring;
- R.sup.6 stands for hydrogen or a C.sub.1-10 acyl group and the salts thereof as well as hydrates of the free compounds of formula (I) and the salts thereof, which comprises hydrolyzing a compound of the formula (II), ##STR14## wherein X is a halide ion, then reacting the obtained salt of the formula (III) ##STR15## wherein Me is a metal atom a) with a racemic or optically active compound of the formula (IV), ##STR16## wherein Y is halogen or arylsulfonyl, or with a compound of the formula (V) ##STR17## then, if desired, acylating the thus obtained active compounds of the formula (I), wherein R.sup.6 stands for hydrogen, to obtain compounds of the formula (I), wherein R.sup.6 is as defined above, except hydrogen; or resolving the racemic compounds of formula (I); or converting the racemic or optionally active compounds of formula (I) to their salts; or liberating the free compounds of formula (I) from their salts; or liberating the free racemic or optically active compounds of formula (I) from their salts.
- 2. A process as claimed in claim 1, which comprises reacting the compounds of formula (III) without isolating them with the compounds of formula (IV) or (V), respectively.
Priority Claims (1)
Number |
Date |
Country |
Kind |
7125/90 |
Nov 1990 |
HUX |
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Parent Case Info
This is a divisional of co-pending application Ser. No. 07/792,255 filed on Nov. 14, 1991, now U.S. Pat. No. 5,179,089.
Non-Patent Literature Citations (1)
Entry |
Harsamyi et al. Chemical Abstracts, vol. 82 No. 156, 275x (1975). |
Divisions (1)
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Number |
Date |
Country |
Parent |
792255 |
Nov 1991 |
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