Title: Talampanel
CAS Registry Number: 161832-65-1
CAS Name: (8R)-7-Acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine
Additional Names: R-(-)-1-(4-aminophenyl)-3-acetyl-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-benzodiazepine
Manufacturers' Codes: LY-300164
Molecular Formula: C19H19N3O3
Molecular Weight: 337.37
Percent Composition: C 67.64%, H 5.68%, N 12.46%, O 14.23%
Literature References: Noncompetitive AMPA receptor antagonist. Prepn: F. Andrasi et al., EP 492485; eidem, US 5536832 (1992, 1996 both to Gyogyszerkutato Intezet KFT). Enantioselective synthesis: I. Ling et al., J. Chem. Soc. Perkin Trans. 1 1995, 1423. HPLC determn in plasma: J. A. Eckstein, S. P. Swanson, J. Chromatogr. B 668, 153 (1995). Stereoselective electropharmacology and neuroprotective effects: D. Lodge et al., Neuropharmacology 35, 1681 (1996). Review of manufacturing process: B. A. Anderson et al. in Process Chemistry in the Pharmaceutical Industry, K. G. Gadamasetti, Ed. (Marcel Dekker, New York, 1999) pp 263-282. Review of clinical development: C. Q. Meng, Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs 1, 637-643 (1999).
Properties: Crystals, mp 169-172°. [a]D -321.34° (c = 1 in methanol).
Melting point: mp 169-172°
Optical Rotation: [a]D -321.34° (c = 1 in methanol)
Therap-Cat: Anticonvulsant.
Keywords: Anticonvulsant; AMPA Receptor Antagonist. |