Malonic acids and esters thereof

Details Malonic acids and esters thereof Malonic acids and esters thereof

1980-10-03

1983-08-09

Helfin, Bernard

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

560 47, 562456, 562434, 549274, C07C 5508, C07C 6938

Patent

active

043980350

ABSTRACT:
The invention concerns the novel compounds dialkyl 2-(3-fluoro-4-nitrophenyl)-2-methylmalonate IIIa and dialkyl 2-(3-fluoro-4-aminophenyl)-2-methylmalonate IVa useful as intermediates in an improved process for making 2-(2-fluoro-4-biphenylyl)propionic acid, known as flurbiprofen, having the formula ##STR1## and ester thereof. It has anti-inflammatory activity which is about 240 times that of aspirin and analgesic activity which is about 180 times that of aspirin in standard laboratory tests. However, despite this high activity, the toxicity (LD.sub.50) is only 1.2 to 2.4 times greater than that of aspirin in standard laboratory tests.
Also within the invention is a novel method of making the above intermediates and analogs thereof useful to prepare corresponding biaryl compounds which have pharmaceutical uses.

REFERENCES:
patent: 3981905 (1976-09-01), Adams et al.
patent: 4266069 (1981-05-01), Walker
patent: 4324904 (1982-04-01), Hylton et al.
Dumaitre et al., "Synthesis and Analgesic and Antiinflammatory Activities of Some Derivatives of 4-Amino-phenylacetic acid and 2-(4-amino-phenyl)Propionic Acid", Eur. J. Med. Chem-Chim. Ther. 14(3), 207-214, (1979), (Current Abstracts of Chemistry vol. 75, Issue 827, 1979).

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