PURPOSE: To provide the subject new compound useful for the prevention, care and treatment of inflammatory diseases in general including intractable dermatopathy owing to its excellent antiinflammatory action and having extremely low side effect.
CONSTITUTION: A 21-substituted steroid compound of formula I (R1 is OH; R2 is H or lower alkyl; X and Y are H or halogen; Z is O or S; wavy line represents that the steric configuration may be α or β), e.g. thioether of betamethazone-21-thiol and N-formyl-L-methionyl-L-leucyl-L-phenylalanine. The compound of formula can be produced by reacting a steroid compound of formula II with 0.1-10 equivalent of N-formylmethionylleucylphenylalanine of formula III and 1-10 equivalent of a dehydrative condensation agent in a solvent (e.g. ethyl acetate) preferably at -10 to +50°C for 30min to 8hr. The dehydrative condensation agent is e.g. N,N'-dicyclohexylcarbodiimide.
SUZUKI YASUTO
MORIOKA TOMONORI
MORIWAKI SHIGERU
HASE TADASHI
TSUCHIYA SHUICHI
