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A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an α-methyl group at the benzylic position to improve potency was found. 3,5-Bis(trifluoromethyl)benzyl bromide has been used as derivatization reagent in detection of uracil in DNA by GC and negative chemical ionization mass spectrometry.
Ho-Jane Shue,; Xiao Chen,; John H. Schwerdt,; Sunil Paliwal,; David J. Blythin,; Lng Lin,; Dalina Cheng Wang,; Gregory A. Reichard,; Hongwu Wang,; John J. Piwinski,; Ruth A. Duffy,; Jean E. Lachowicz,; Vicki L. Coffin,; Amin A. Nomeir,; Cynthia A. Morgan.Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions. Bioorganic & Medicinal Chemistry Letters. 2006, 16(14) ,1065-1069.
Igor Kazmierski,; Mylène Bastienn,; Corinne Gosmini,; Jean-Marc Paris,; Jacques Périchon. Convenient Processes for the Synthesis of Aromatic Ketones from Aryl Bromides and Carboxylic Anhydrides Using a Cobalt Catalysis. J. Org. Chem. 2004, 69(3),936-942.
Hazard Statements: H314-H318
Causes severe skin burns and eye damage. Causes serious eye damage.
Precautionary Statements: P260u-P303+P361+P353-P305+P351+P338-P301+P330+P331-P405-P501a
Do not breathe dusts or mists. IF ON SKIN (or hair): Remove/Take off immediately all contaminated clothing. Rinse skin with water/shower. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. Store locked up. Dispose of contents/container in accordance with local/regional/national/international regulations.