Title:
NEW STEROID DERIVATIVES OF PREGNA-1,4-DIENE-3,20-DIONE, THEIR PRODUCTION, PRODUCTION OF SUBSTITUTED 16,17-METHYLENEDIOXY DERIVATIVES AND THEIR USE AND NEW INTERMEDIATES
Document Type and Number:
Japanese Patent JP3172575
Kind Code:
B2
Abstract:
PURPOSE: To provide a compd. useful for production of a budesonide and desonide.
CONSTITUTION: The compd. of formula I (R is H, a 1 to 8C acyl, etc.). For example, (11β.16α)-21-(acetyloxy)-11-(formyloxy-16,17-[(1-methylethylidene)bis(oxy)]pregna-1,4-diene-3,20-dione. The compd. of the formula I is obtd. by treating, for example, a compd. of formula II with a chlorinating or brominating agent (e.g.: N-chloroacetamide, N-chlorosuccinimide, etc.), and formyloxylating agent (e.g. dimethylformamide, etc.), in acidic medium to obtain the compd. of formula III (Hal is Cl, Br), treating this compd. with an acetone in the presence of a strong acid (more preferably perchloric acid, etc.), and in the presence of a dehydrating agent (more preferably isopropyl acetate) to obtain the compd. of formula IV, then subjecting this compd. to dehalogenation by the effect of tributyltin hydride in the presence of a free radical reaction initiator.
Inventors:
Luk Dovocel
Philip Makiewich
Philip Makiewich
Application Number:
JP11520192A
Publication Date:
June 04, 2001
Filing Date:
April 09, 1992
Export Citation:
Assignee:
Hoechst Marion Roussel
International Classes:
A61K31/57; B01J27/10; C07B61/00; C07J5/00; C07J71/00; (IPC1-7): C07J71/00; A61K31/57; B01J27/10; C07J5/00
Domestic Patent References:
| JP4994660A |
Attorney, Agent or Firm:
Motohiro Kurauchi (1 outside)