146137-80-6Relevant articles and documents
Loxoprofen derivative
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Paragraph 0035-0036; 0038, (2019/01/23)
The invention provides a Loxoprofen derivative. Gastrointestinal tract side effects are low, and the bioavailability can be improved.
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl) methyl]phenyl}propanoic acid: Nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities
Yamakawa, Naoki,Suemasu, Shintaro,Matoyama, Masaaki,Kimoto, Ayumi,Takeda, Miho,Tanaka, Ken-Ichiro,Ishihara, Tomoaki,Katsu, Takashi,Okamoto, Yoshinari,Otsuka, Masami,Mizushima, Tohru
scheme or table, p. 7879 - 7882 (2011/02/22)
We previously proposed that membrane permeabilization activity of NSAIDs is involved in NSAID-induced gastric lesions. We here synthesized derivatives of loxoprofen that have lower membrane permeabilization activity than other NSAIDs. Compared to loxoprofen, the derivatives 10a and 10b have lower membrane permeabilization activity and their oral administration produced fewer gastric lesions but showed an equivalent anti-inflammatory effect. These results suggest that 10a and 10b are likely to be therapeutically beneficial as safer NSAIDs.
Method for producing halogen-substituted aromatic aldehyde
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Page/Page column 6, (2008/06/13)
In the production method of the invention, a halogen-substituted aromatic compound is reacted with carbon monoxide in the presence of hydrogen fluoride and boron trifluoride into a corresponding halogen-substituted aromatic aldehyde. By the use of hydrogen fluoride and boron trifluoride, the para position to halogen atom is selectively formylated to provide the halogen-substituted aromatic aldehyde in high yields in a short reaction time even at temperatures lower than room temperature.