41292-86-8Relevant academic research and scientific papers
Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage
Perissutti, Elisa,Fiorino, Ferdinando,Renner, Christian,Severino, Beatrice,Roviezzo, Fiorentina,Sautebin, Lidia,Rossi, Antonietta,Cirino, Giuseppe,Santagada, Vincenzo,Caliendo, Giuseppe
, p. 7774 - 7780 (2006)
Novel substituted 2-methyl-3-indolylacetic derivatives were synthesized and evaluated for their activity in vitro and in vivo on COX-1 and COX-2. Active compounds were screened to determine their gastrointestinal tolerability in vivo in the rat. Results s
Hydrogen-Borrowing Amination of Secondary Alcohols Promoted by a (Cyclopentadienone)iron Complex
Aiolfi, Francesco,Bai, Xishan,Cettolin, Mattia,Dal Corso, Alberto,Gennari, Cesare,Piarulli, Umberto,Pignataro, Luca
, p. 3545 - 3555 (2019/09/09)
Thanks to a highly active catalyst, the scope of the (cyclopentadienone)iron complex-promoted 'hydrogen-borrowing' (HB) amination has been expanded to secondary alcohols, which had previously been reported to react only in the presence of large amounts of co-catalysts. A range of cyclic and acyclic secondary alcohols were reacted with aromatic and aliphatic amines giving fair to excellent yields of the substitution products. The catalyst was also able to promote the cyclization of diols bearing a secondary alcohol group with primary amines to generate saturated N-heterocycles.
Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain
Vardanyan, Ruben,Vijay, Gokhale,Nichol, Gary S.,Liu, Lu,Kumarasinghe, Isuru,Davis, Peg,Vanderah, Todd,Porreca, Frank,Lai, Josephine,Hruby, Victor J.
experimental part, p. 5044 - 5053 (2009/12/04)
Acids 9a-f as possible bivalent ligands designed as a structural combination of opioid μ-agonist (Fentanyl) and NSAID (Indomethacin) activities and produced compounds which were tested as analgesics. The obtained series of compounds exhibits low affinity and activity both at opioid receptors and as cyclooxygenase (COX) inhibitors. One explanation of the weak opioid activity could be stereochemical peculiarities of these bivalent compounds which differ significantly from the fentanyl skeleton. The absence of significant COX inhibitory properties could be explained by the required substitution of an acyl fragment in the indomethacin structure for 4-piperidyl.
Aminohaloborane in Organic Synthesis. IX. Exclusive ortho Acylation Reaction of N-Monoaminoalkylanilines
Adachi, Makoto,Sasakura, Kazuyuki,Sugasawa, Tsutomu
, p. 1826 - 1835 (2007/10/02)
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
