9503. Tofisopam

Nomenclature

CAS number: 22345-47-7
1-(3,4-Dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine; EGYT-341; Grandaxin (EGYT); Seriel (Biogalenique).
C22H26N2O4; mol wt 382.45.
C 69.09%, H 6.85%, N 7.32%, O 16.73%.

Description and references

The first 5H-2,3-benzodiazepine. Prepn: J. Korosi et al., HU 155572 (1969 to Pharm. Res. Inst.), C.A. 70, 115026a (1969); GB 1202579 corresp to US 3736315 (1970, 1973 both to EGYT); J. Korosi, T. Lang, Ber. 107, 3883 (1974). Synthesis and conformation: eidem, Ther. Hung. 23, 132 (1975). FT 13C NMR study: A. Neszmelyi et al., Ber. 107, 3894 (1974). Pharmacology: L. Petocz, I. Kosoczky, Ther. Hung. 23, 134 (1975). Human pharmacokinetics: S. Ronai et al., ibid. 139. Comparative efficacy: H. L. Goldberg, R. J. Finnerty, Am. J. Psychiatry 136, 196 (1979).

Chemical structure

Properties

Colorless to light cream cryst powder from isopropyl alcohol, mp 156-157°. uv max (methanol): 310, 272, 239 nm (ε 16100, 11200, 26300).

Therapeutic Category

Anxiolytic.

Keywords

Anxiolytic; Benzodiazepine Derivatives