Etiprednol dicloacetate, a new soft glucocorticoid drug candidate. Development of chemistry.
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.
Csanádi
A
A
IVAX Drug Research Institute Ltd., Budapest, Hungary.
Horváth
Gy
G
Szekeres
T
T
Haskó
T
T
Ila
L
L
Ivanics
J
J
Patthy
M
M
Salát
J
J
Seres
G
G
Pallagi
I
I
Tóth
G
G
Szederkényi
F
F
Kónya
A
A
Tegdes
A
A
Bodor
N
N
Zubovics
Z
Z
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
D000305:Adrenal Cortex Hormones; D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D007202:Indicators and Reagents; D012997:Solvents; C450000:etiprednol dicloacetate