title: Etiprednol dicloacetate, a new soft glucocorticoid drug candidate. Development of chemistry.
abstract: During development of chemistry of the soft drug candidate etiprednol dicloacetate (BNP-166) 1) optimization studies on the three-step chemical synthesis resulted in a process that could be scaled-up to the kg level, 2) the impurity profile was determined, 3) synthetic routes were developed for the preparation of the radiolabeled target compound, and 4) a series of hydroxylated metabolites was prepared.
authors.affiliation: IVAX Drug Research Institute Ltd., Budapest, Hungary.
authors.forename: A
authors.initials: A
authors.lastname: Csanádi
authors.forename: Gy
authors.initials: G
authors.lastname: Horváth
authors.forename: T
authors.initials: T
authors.lastname: Szekeres
authors.forename: T
authors.initials: T
authors.lastname: Haskó
authors.forename: L
authors.initials: L
authors.lastname: Ila
authors.forename: J
authors.initials: J
authors.lastname: Ivanics
authors.forename: M
authors.initials: M
authors.lastname: Patthy
authors.forename: J
authors.initials: J
authors.lastname: Salát
authors.forename: G
authors.initials: G
authors.lastname: Seres
authors.forename: I
authors.initials: I
authors.lastname: Pallagi
authors.forename: G
authors.initials: G
authors.lastname: Tóth
authors.forename: F
authors.initials: F
authors.lastname: Szederkényi
authors.forename: A
authors.initials: A
authors.lastname: Kónya
authors.forename: A
authors.initials: A
authors.lastname: Tegdes
authors.forename: N
authors.initials: N
authors.lastname: Bodor
authors.forename: Z
authors.initials: Z
authors.lastname: Zubovics
mesh_terms: D000305:Adrenal Cortex Hormones / Q000737:chemistry*; D000893:Anti-Inflammatory Agents / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D005938:Glucocorticoids / Q000737:chemistry*; D007202:Indicators and Reagents; D007553:Isotope Labeling; D009682:Magnetic Resonance Spectroscopy; D012997:Solvents
chemical_list: D000305:Adrenal Cortex Hormones; D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D007202:Indicators and Reagents; D012997:Solvents; C450000:etiprednol dicloacetate