Document Type and Number:
Japanese Patent JPS5614677
Kind Code:
B2
Abstract:
1499822 2 - Bromo - 6# - fluoropregna- 1,4-diene-3,20-diones PIERREL SpA 6 Feb 1975 [27 Feb 1974 5 July 1974 25 July 1974 19 Nov 1974] 8928/74 29984/74 32945/74 and 49982/74 Heading C2U Novel steroids have the formula wherein either X is OH and Y is F, Cl or Br, or X and Y are each Cl, and (i) R 1 is OH, R 2 is OH and R 3 is H, α-CH 3 or #-CH 3 ; or (ii) R 1 is acyloxy, R 2 is OH and R 3 is H, α-acyloxy, α-CH 3 or #-CH 3 ; or (iii) R 1 is OH or acyloxy, R 2 is acyloxy and R 3 is H, α-ChH 3 or #-CH 3 ; or (iv) R 1 is OH or acyloxy and either R 2 is OH and R 3 is α-OH or R 2 , and R 3 together are wherein R 4 is H or hydrocarbyl and R 5 is hydrocarbyl; or (v) R 1 and R 2 together are wherein R 6 is H, hydrocarbyl or alkoxy and R 7 is hydrocarbyl, and R 3 is H, α-CH 3 or #-CH 3 . They may be prepared as illustrated in the following reaction scheme which is largely self-explanatory. (XI)#(XIV) is the reaction of a 17α-acetoxy-16-unsubstituted compound with KOAc in hot DMF. 17α- Esters are prepared from 17α,21-diols via 17,21- o - esters. 17,21 - Acetonides are prepared from the 17α,21-diols and 2,2-dimethoxypropane. The novel steroids have anti-inflammatory activity and they may be made up into pharmaceutical compositions with suitable carriers.
Application Number:
JP2298075A
Publication Date:
April 06, 1981
Filing Date:
February 26, 1975
Export Citation:
International Classes:
A61K31/57; A61P29/00; C07J5/00; C07J21/00; C07J71/00