8226. Rimexolone

Nomenclature

CAS number: 49697-38-3
(11β,16α,17β)-11-Hydroxy-16,17-dimethyl-17-(1-oxopropyl)androsta-1,4-dien-3-one; 11β-hydroxy-16α,17α-dimethyl-17-propionylandrosta-1,4-dien-3-one; 11β-hydroxy-16α,17α,21-trimethylpregna-1,4-diene-3,20-dione; trimexolone; Org-6216; Rimexel (Organon); Vexol (Alcon).
C24H34O3; mol wt 370.52.
C 77.80%, H 9.25%, O 12.95%.

Description and references

Prepn: NL 7300313; G. F. Woods et al., US 3947478 (1973, 1976 both to Akzo); J. Cairns et al., J. Chem. Soc. Perkin Trans. 1 1981, 2306. Pharmacology: P. K. Fox et al., Arzneim.-Forsch. 30, 55 (1980). Clinical trial in rheumatoid arthritis: E. van Vliet-Daskalopoulou et al., Br. J. Rheumatol. 26, 450 (1987). Clinical pharmacokinetics: G. Gevers et al., Clin. Rheumatol. 13, 103 (1994).

Chemical structure

Properties

Crystals, mp 258-268°. [α]D +100° (c = 0.92 in pyridine). uv max: 244 nm (ε 14600).

Therapeutic Category

Anti-inflammatory (local).

Keywords

Glucocorticoid