IT1237444B - 6-Alpha-halo-9,11-oxido-pregna-1,4-diene derivs. prepn. - by halogenation of 3-alkoxy or acyloxy-1,3,5-tri:ene prepd. by acylation of etherification of 3-keto 9,11-oxido-pregna-1,4-diene - Google Patents
6-Alpha-halo-9,11-oxido-pregna-1,4-diene derivs. prepn. - by halogenation of 3-alkoxy or acyloxy-1,3,5-tri:ene prepd. by acylation of etherification of 3-keto 9,11-oxido-pregna-1,4-dieneInfo
- Publication number
- IT1237444B IT1237444B IT2204979A IT2204979A IT1237444B IT 1237444 B IT1237444 B IT 1237444B IT 2204979 A IT2204979 A IT 2204979A IT 2204979 A IT2204979 A IT 2204979A IT 1237444 B IT1237444 B IT 1237444B
- Authority
- IT
- Italy
- Prior art keywords
- halo
- alpha
- pregna
- diene
- derivs
- Prior art date
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- Steroid Compounds (AREA)
Abstract
Prepn. of 6 alpha-halo-3-keto-pregna-1,4-diene derivs of formula (III) comprises reaction of 3-keto-pregna-1,4-diene derivs. (I) with an acylating or etherifying agent (such as acyl anhydrides, isopropenyl acetate or trialkyl orthoformates) in the presence of acid catalysts (such as p-toluene sulphonic acid)to give novel corresp. 3-enol deriv. of formula (II), and reaction of this with an appropriate halogenating agent. (such as a N-halo-amide or perchloryl fluoride). (where R,Z=H, hydroxy or =9C carboxylic acyloxy or W and Z together may be -O-CMe2-O--W=H hydroxy or methyl, X= halo pref. Cl or F and R1=lower alkyl or lower acyl) The cpds are useful as intermediates. The epoxy ring may be opened by reaction with hydrohalic acids to give the 6alpha, 9alpha-dihalo-11-beta-hydroxy-pregna-1,4-diene-3-one derivs. The 9 halo cpd. (not 9-F) may be dehalogenated by known methods. Typical products prepared from (III) include fluocinonide which may be deacylated to give fluocinolone acetonide, 6 alpha, 9 alpha-difluoro prednisolone, flumethasone, flurisolide, diflucortolone, diflorasone etc. The process gives (II) as te 6-alpha-halo epimer or a mixture in which the 6 alpha-epimer predominates.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT2204979A IT1237444B (en) | 1979-04-23 | 1979-04-23 | 6-Alpha-halo-9,11-oxido-pregna-1,4-diene derivs. prepn. - by halogenation of 3-alkoxy or acyloxy-1,3,5-tri:ene prepd. by acylation of etherification of 3-keto 9,11-oxido-pregna-1,4-diene |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT2204979A IT1237444B (en) | 1979-04-23 | 1979-04-23 | 6-Alpha-halo-9,11-oxido-pregna-1,4-diene derivs. prepn. - by halogenation of 3-alkoxy or acyloxy-1,3,5-tri:ene prepd. by acylation of etherification of 3-keto 9,11-oxido-pregna-1,4-diene |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IT7922049A0 IT7922049A0 (en) | 1979-04-23 |
| IT1237444B true IT1237444B (en) | 1993-06-05 |
Family
ID=11190713
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IT2204979A IT1237444B (en) | 1979-04-23 | 1979-04-23 | 6-Alpha-halo-9,11-oxido-pregna-1,4-diene derivs. prepn. - by halogenation of 3-alkoxy or acyloxy-1,3,5-tri:ene prepd. by acylation of etherification of 3-keto 9,11-oxido-pregna-1,4-diene |
Country Status (1)
| Country | Link |
|---|---|
| IT (1) | IT1237444B (en) |
-
1979
- 1979-04-23 IT IT2204979A patent/IT1237444B/en active
Also Published As
| Publication number | Publication date |
|---|---|
| IT7922049A0 (en) | 1979-04-23 |
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| TA | Fee payment date (situation as of event date), data collected since 19931001 |
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