9284. Theofibrate

Nomenclature

CAS number: 54504-70-0
2-(4-Chlorophenoxy)-2-methylpropanoic acid 2-(1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-7H-purin-7-yl)ethyl ester; 2-(p-chlorophenoxy)-2-methylpropionic acid ester with 7-(2-hydroxyethyl)theophylline; 1-(theophyllin-7-yl)ethyl 2-(p-chlorophenoxy)isobutyrate; etofylline clofibrate; ML-1024; Duolip (Merckle).
C19H21ClN4O5; mol wt 420.85.
C 54.22%, H 5.03%, Cl 8.42%, N 13.31%, O 19.01%.

Description and references

Deriv of clofibric acid, q.v., with antilipemic, antithrombotic, and platelet-aggregation inhibitory activity: Prepn: G. Metz, M. Specker, DE 2308826; eidem, US 3984413 (1974, 1976 both to Merckle); eidem, Arzneim.-Forsch. 25, 1686 (1975). Hypolipemic activity: G. Metz et al., ibid. 27, 1173 (1977). Series of articles on chemistry, biopharmaceutic evaluation, pharmacology, toxicology, clinical studies: ibid. 30, 2013-2074 (1980).

Chemical structure

Properties

Colorless crystals from ethanol, mp 133-135°. Practically insol in water at pH 2-7.4 and in cold alcohols. Sol in acetone, chloroform, hot alcohols. LD50 in mice, rats, dogs (g/kg): 11.7, 17.0, >10.0 orally (Metz et al.).

Therapeutic Category

Antilipemic.

Keywords

Antilipemic; Fibrates