5484. Lidoflazine

Nomenclature

CAS number: 3416-26-0
4-[4,4-Bis(4-fluorophenyl)butyl]-N-(2,6-dimethylphenyl)-1-piperazineacetamide; 4-[4,4-bis(p-fluorophenyl)butyl]-1-piperazineaceto-2′,6′-xylidide; 1-[4,4-di(4-fluorophenyl)butyl]-4-[(2,6-dimethylanilinocarbonyl)methyl]piperazine; McN-JR-7094; R-7904; Angex (Janssen); Clinium (McNeil); Klinium (Janssen); Ordiflazine; Corflazine (Daltan).
C30H35F2N3O; mol wt 491.62.
C 73.29%, H 7.18%, F 7.73%, N 8.55%, O 3.25%.

Description and references

Calcium blocking agent. Prepn: NL 6507312; H. K. F. Hermans, W. K. Schaper, US 3267104 (1965, 1966, both to Janssen). Crystal structure: G. Germain et al., Acta Crystallogr. 33B, 1971 (1977). Tissue specificity of calcium-blocking properties: J. M. Van Neuten, D. Wellens, Arch. Int. Pharmacodyn. Ther. 242, 329 (1979). Cardioprotective effects: W. Daenen, W. Flameng, Angiology 32, 543 (1981). Effects in angina: F. L. Gobel et al., Circulation 65, 1 Pt. 2, 127 (1982); W. Shapiro et al., ibid. 143.

Chemical structure

Properties

Crystals, mp 159-161°. Almost insol in water (<0.01%), very sol in chloroform (>50%), but much less sol in other common organic solvents: W. K. Schaper et al., J. Pharmacol. Exp. Ther. 152, 265 (1966).

Therapeutic Category

Vasodilator (coronary).

Keywords

Calcium Channel Blocker; Piperazine Derivatives; Vasodilator (Coronary)