Diflucortolone
Structural Formula Vector Image
Title: Diflucortolone
CAS Registry Number: 2607-06-9
CAS Name: (6a, 11b, 16a)-6,9-Difluoro-11,21-dihydroxy-16-methylpregna-1,4-diene-3,20-dione
Additional Names: 6a,9a-difluoro-16a-methyl-1,4-pregnadiene-11b,21-diol-3,20-dione; 6a,9a-difluoro-16a-methyl-1-dehydrocorticosterone
Molecular Formula: C22H28F2O4
Molecular Weight: 394.45
Percent Composition: C 66.99%, H 7.15%, F 9.63%, O 16.22%
Literature References: The 9a-fluoro deriv of fluocortolone, q.v. Prepn: BE 639708; K. Kieslich et al., US 3426128 (1964, 1969, both to Schering AG); eidem, Arzneim.-Forsch. 26, 1462 (1976). Toxicity: P. Gunzel et al., ibid. 1476. Series of articles on pharmacology, toxicity, metabolism and clinical studies: ibid. 26, 1463-1513 (1976).
Properties: Crystals from ethyl acetate-ether, mp 240-244°. uv max: 237 nm (e 16600) (Kieslich, 1969). Also reported as mp 248-249°. [a]D22 +111° (methanol) (Kieslich, 1976).
Melting point: mp 240-244°; mp 248-249°
Optical Rotation: [a]D22 +111° (methanol) (Kieslich, 1976)
Absorption maximum: uv max: 237 nm (e 16600) (Kieslich, 1969)
 
Derivative Type: 21-Valerate
CAS Registry Number: 59198-70-8
Trademarks: Neribas (Schering AG); Neriforte (Schering AG); Nerisona (Schering AG); Nerisone (Schering AG); Temetex (Sauter); Texmeten (Roche)
Molecular Formula: C27H36F2O5
Molecular Weight: 478.57
Percent Composition: C 67.76%, H 7.58%, F 7.94%, O 16.72%
Properties: Crystals, mp 195-195.5°. [a]D22 +100.8° (dioxane). Approx LD50 in mice, rats: >4, 3.1 g/kg orally; 180, 13 mg/kg s.c.; 450, 98 mg/kg i.p. (Gunzel).
Melting point: mp 195-195.5°
Optical Rotation: [a]D22 +100.8° (dioxane)
Toxicity data: Approx LD50 in mice, rats: >4, 3.1 g/kg orally; 180, 13 mg/kg s.c.; 450, 98 mg/kg i.p. (Gunzel).
 
Therap-Cat: Anti-inflammatory.
Keywords: Glucocorticoid.

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