4209-65-8Relevant articles and documents
SMALL MOLECULE BRADYKININ B1 RECEPTOR ANTAGONISTS
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Page/Page column 81, (2009/04/25)
Disclosed are compounds of formula (I) which are bradykinin B1 receptor (B1R) antagonists. These compounds are useful to treat diseases or relieve adverse symptoms associated with inflammation and pain. The invention encompasses novel compounds and acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases involving inflammation and pain.
Chelating diamide based rate enhancement of intramolecular alkene hydroaminations catalyzed by a neutral Sc(III) complex
Joon, Young Kim,Livinghouse, Tom
, p. 4391 - 4393 (2007/10/03)
(Chemical Equation Presented) Neutral scandium amido complexes are viable catalysts for intramolecular alkene hydroamination. Catalytic activity is strongly coupled to the electronic character of the Sc(III) ligand environment with chelating diamide coord
3- Or 4-monosubstituted phenol derivatives useful as H3 ligands
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Page/Page column 95, (2010/02/14)
The invention relates to 3- or 4-monosubstituted phenol derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said 3- or 4-monosubstituted phenol derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Asymmetric syntheses of 2-substituted and 2,5-disubstituted pyrrolidines from (3S,5R,7aR)-5-(benzotriazol-1-yl)-3-phenyl[2,1-b]oxazolopyrrolidine
Katritzky, Alan R.,Cui, Xi-Lin,Yang, Baozhen,Steel, Peter J.
, p. 1979 - 1985 (2007/10/03)
Benzotriazole, 2,5-dimethoxytetrahydrofuran, and (S)-phenylglycinol in one step gave 80% of (3S, 5R,7aR)-5-(benzotriazol-1-yl)-3-phenyl-[2,1- b]oxazolopyrrolidine (6), whose crystal structure was confirmed by X-ray crystallography. Novel chiral pyrrolidine synthon 6 reacts with organosilicon (allyltrimethylsilanes and vinyloxytrimethylsilanes), organophosphorus, organozinc, and Grignard reagents to afford chiral 2-substituted and 2,5- disubstituted pyrrolidines.
Diastereoselective synthesis of 2,5-dimethylpyrrolidines and 2,6- dimethylpiperidines by reductive amination of 2,5-hexanedione and 2,6- heptanedione with hydride reagents
Boga,Manescalchi,Savoia
, p. 4709 - 4722 (2007/10/02)
The reductive amination of 2,5-hexanedione and 2,6-heptanedione with ammonia and primary amines in the presence of hydride reagents afforded 2,5- dimethylpyrrolidines and 2,6-dimethylpiperidines with variable diastereoselectivity, as the cis/trans ratio was affected by the size of the ring formed and the steric and electronic properties of the nitrogen substituent. Increasing the bulkiness of the nitrogen substituent, the cis pyrrolidines and the trans-piperidines were obtained with enhanced selectivity.
Catalytic Hydrogenation of Pyrroles at Atmospheric Pressure
Kaiser, Hans-Peter,Muchowski, Joseph M.
, p. 4203 - 4209 (2007/10/02)
N-(tert-Butoxycarbonyl)pyrroles are catalytically hydrogenated to the corresponding pyrrolidines, over 5percent platinum on carbon catalyst, at room temperature and atmospheric pressure.Under these conditions O-benzyl groups are retained and 2,5-disubstit