Processes for the preparation of hydratropic acids and esters

Details Processes for the preparation of hydratropic acids and esters Processes for the preparation of hydratropic acids and esters

1979-12-19

1981-05-05

Trousof, Natalie

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

Organic compounds

Carboxylic acid esters

2603402, 260465D, 560 19, 560 21, 560 22, 560 23, 560 45, 560 47, 560 48, C07C 7946

Patent

active

042660696

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: 3068266 (1962-12-01), Wilkinson et al.
patent: 3240824 (1966-03-01), Boudakian et al.
patent: 3701814 (1972-10-01), Shilling
patent: 3860598 (1975-01-01), Rosenkranz et al.
patent: 4007179 (1977-02-01), Yoshida
Carney et al., Experientia 29/8, A Potent Non-Steroidal Anti-Inflammatory Agent, p. 938, 1973.
Makosza et al., Roczniki Chem., 50, 1841, 1976.
House, Modern Synthetic Reactions, W. A. Benjamin, Inc., 2d edition, pp. 510-513, 1972.

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