Process for the preparation of optically active 2-aryl-alkanoic acids, especially 2-aryl-propionic acids
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United States of America Patent
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Nov 30, 1993
Issued Date -
N/A
app pub date -
Feb 27, 1990
filing date -
May 16, 1989
priority date (Note) -
Expired
status (Latency Note)
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Abstract
A chemical process is disclosed for the preparation of a pharmaceutically active compound in an enantiomeric form either (R) or (S) of the structure ##STR1## and a suitable pharmaceutical salt, e.g. alkali or earth metal, D-glucamine or D-ribamine, where R.sub.1 represents an optionally substituted aryl group same as phenyl or naphthyl group, optionally including a heterocyclic ring system, which is optionally substituted, or represents a hetero-aromatic ring system optionally containing in addition to carbon atoms one or more atoms selected from the group consisting of nitrogen and oxygen; the enantiomeric R or S-compounds of (I) are obtained from a suitable ketone (II) by reduction with an LiAlH.sub.4.sup.-'chiraldid-complex' to the corresponding S- or R-alcohol, following chlorination with retention of configuration, and producing a steriochemical pure R or S magnesium organic compound by subsequent carbonation with carbon dioxide in the presence of a ligand by keeping the stereochemical configuration R or S at 98% enantiomeric excess at least including high yields, and if desired converting compounds (I) into a pharmaceutically acceptable salt or ester thereof. Especially pharmaceutically complexes with D-glucamine and D-ribamine in a stoichiometric ratio of 1:1, including salts comprised of N-cationic detergents with 2-(S)-aryl-alkanoic acids.

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- 2 Other
Patent Owner(s)
Patent Owner | Address | |
---|---|---|
MEDICE LTD CHEM -PHARM FABRIK PUTTER GMBH & CO KG KUHLOWEG 37-39 D-5860 ISERLOHN A CORP OF GERMANY | Not Provided |
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- Non-US Classification not provided for expired patents
Inventor(s)
Inventor Name | Address | # of filed Patents | Total Citations |
---|---|---|---|
Hanna, Samir B | Rolla, MO | 2 | 16 |
Paradies, Henrich H | Iserlohn, DE | 18 | 95 |
Schneider, Bernd | Iserlohn, DE | 52 | 803 |
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Maintenance Fees
Fee | Large entity fee | small entity fee | micro entity fee | due date |
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Fee | Large entity fee | small entity fee | micro entity fee |
---|---|---|---|
Surcharge after expiration - Late payment is unavoidable | $700.00 | $350.00 | $175.00 |
Surcharge after expiration - Late payment is unintentional | $1,640.00 | $820.00 | $410.00 |
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