Processes for the preparation of hydratropic acids and esters
US4324904A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 19, 1979 |
| Grant date | Apr 13, 1982 |
| Priority date | — |
| Expiry date | Dec 19, 1999 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C51/38
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.