205442-92-8Relevant academic research and scientific papers
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.
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.
A short asymmetric synthesis of 2,5-disubstituted pyrrolidines
Katritzky, Alan R.,Cui, Xi-Lin,Yang, Baozhen,Steel, Peter J.
, p. 1697 - 1700 (2007/10/03)
A novel approach to chiral 2,5-disubstituted pyrrolidines, starting from chiral 2-phenyl-glycimol, 1,5-dimethoxytetrahydrofuran, and benzotriazole, involves the diastereoselective substitution by Grignard reagents of a benzotriazolyl group in a crystalline intermediate obtained in high yield.
