PURPOSE: To provide the subject new confound useful as an antiinflammatory agent hardly having no side effect.
CONSTITUTION: A compound of formula I (either of R1, R2 is group of formula II, but when R1 is the group of formula II, R2 is OH, and when R2 is the group of formula II, R1 is OH, 1-6C acyloxy, organic sulfonyloxy. halogen; R3 is H, lower alkyl; X1, X2 are H, halogen; the wave line can take both of α,β- configurations; n is 1-6). For example, 9-fluoro-17-[4-(2-formylamino-4- methylthiobutyryloxy)-butyryloxy]11β, 21-dihydroxy-16β-methylpregna-1,4- diene-3,20-dione. The compound of formula I is obtained by reacting a 17- halogenated alkyl carboxylic acid ester steroid of formula III (Y is halogen) with N-formylmethionine of formula IV in the presence of a base.
SUZUKI YASUTO
MORIOKA TOMONORI
MORIWAKI SHIGERU
HASE TADASHI
TSUCHIYA SHUICHI