EASILY ABSORBABLE PRODRUG OF HALOGENNCONTAINING GLUCOCORTICOSTEROID AND ITS DRUG COMPOSITION

摘要

NEW MATERIAL:A compound of formula I: [R1 and R11 are H, F, or Cl; R2 is OH, -OCOR7 R7 is H, etc.); R3 and R4 are H or 1-8C alkyl groups; R5 is H or -COOR7 group; R6 is OH, F, etc.; R9 is H, 1-8C alkyl group, etc.; the compound may be a pharmaceutically acceptable salt when R10 is H; Z is oxo, beta-OH, etc.; the broken line may be double bond; the wavy line is alpha-or beta-coordination]. EXAMPLE:21-Acetyloxy-9alpha-fluoro-11beta, 17alpha-dihydroxypregn-4-en-20-one-3,2'- spiro(4'-carbethoxy-1',3'-thiazolidine). USE:Anti-inflammatory drugs, and easily absorbable prodrugs. PROCESS:A compound of formula I wherein the 3-position is keto group is reacted with a compound of formula II in the presence of an organic base in an organic solvent, if necessary, the base itself as a solvent, to give the objective compound of formula I.