- 4- ARYL(PIPERIDIN-4-YL)] AMINOBENZAMIDES WHICH BIND TO THE DELTA-OPIOID RECEPTOR
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4-[aryl(piperidin-4-yl)] aminobenzamides are delta-opioid receptor agonists/antagonists of formula (I). As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their agonist/antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of mental illness, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents, and agents for the treatment of respiratory diseases. In formula (I), [Ar is phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted with 1 to 3 R; R - R are described in the application].
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Page/Page column 16-17
(2008/06/13)
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- Aminohaloborane in Organic Synthesis. IX. Exclusive ortho Acylation Reaction of N-Monoaminoalkylanilines
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The exclusive ortho acylation reaction of aniline derivatives using boron trichloride made possible the one-step synthesis of 2-acyl-N-monoaminoalkylanilines (1) and the corresponding imines (2) from N-monoaminoalkylanilines, even in the case of compounds with a bulky substituent at the nitrogen atom.Conventional methods only give 1 via elaborate procedures.Keywords: regioselective reaction; 2-acylaniline derivative; 2-acylaniline-imine derivative; boron trichloride
- Adachi, Makoto,Sasakura, Kazuyuki,Sugasawa, Tsutomu
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p. 1826 - 1835
(2007/10/02)
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