Title:
NEW PREPARATION PROCESS OF 16ALPHA-METHYLATED STEROID
Document Type and Number:
Japanese Patent JP3535555
Kind Code:
B2
Abstract:
PURPOSE: To obtain compounds used for anti-inflammatory or the like with high efficiency by, after treating specific steroid derivatives with a methylating agent in the presence of a copper-based catalyst, hydrolyzing the formed 16α- methylated enolate and reacting the formed enol with an oxidating agent.
CONSTITUTION: Steroid base compounds of formula I are treated with a methylating agent in the presence of a copper-based catalyst to form 16α-methylated enolate. Subsequently, after hydrolyzing the product to form corresponding enol, the obtained enol is reacted with an oxidating agent to obtain the object 16α-methylated steroids useful as an anti-inflammatory or as a potential precursor. In formula I, rings A, B are each residual groups of formula II (wherein R3 is H, F, methyl; ketone on 3rd position can be protected) or the like; R is methyl, formula CH2OR' (R' is H, an ether residual group, an ester residual group); R1 is H, a (protected) hydroxy functional group; R2 is a hydroxy functional group, F, Br or the like; R1 and R2 together form a second bond, epoxide.
Inventors:
Roussel, Patrick
Vivat, Michel
Vivat, Michel
Application Number:
JP1776294A
Publication Date:
June 07, 2004
Filing Date:
January 19, 1994
Export Citation:
Assignee:
Roussel, Uclaf
International Classes:
C07B61/00; C07J5/00; C07J7/00; C07J71/00; C07J75/00; (IPC1-7): C07J7/00; C07J5/00; C07J75/00
Attorney, Agent or Firm:
倉内 基弘 （外１名）