- A preparation method of budesonide
-
The invention discloses a budesonide preparing method. Prednisone I and acetic anhydride II react to produce 17,21-diacetoxy-1,4-pregnane diene-3,11,20-triketone III, the III is degreased in an anhydrous solvent to obtain 21-acetoxyl group-1,4,16-pregnane diene-3,11,20-triketone IV, the IV is oxidized to obtain 16alpha,17alpha-dyhydroxy-21-acetoxyl-1,4-pregnane diene-3,11,20-triketone V, the V and n-butyl aldehyde VI are condensed to obtain 16alpha,17alpha-22(R,S) propyl methylenedioxy-21-acetoxyl group-1,4-pregnane diene-3,11,20-triketone VII, the VII is reduced to obtain 16alpha,17alpha-22(R,S) propyl methylenedioxy-11beta-hydroxyl-21-acetoxyl group-1,4-pregnane diene-3,20-diketone VIII, the VIII is subjected to base catalysis to obtain budesonide IX. The budesonide preparing method is suitable for industrial production.
- -
-
Paragraph 0049; 0050; 0051; 0067; 0078
(2017/08/25)
-
- ISOXAZOLIDINE DERIVATIVES
-
Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.
- -
-
Page/Page column 37
(2012/09/25)
-
- ISOXAZOLIDINE DERIVATIVES
-
The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of isoxazolidine.
- -
-
Page/Page column 85-86
(2012/10/07)
-
- ISOXAZOLIDINE DERIVATIVES
-
The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of isoxazolidine.
- -
-
Page/Page column 43
(2011/04/18)
-
- ISOXAZOLIDINE DERIVATIVES
-
Novel glucocorticosteroids that are derivatives of isoxazolidine are useful as anti-inflammatory and antiallergic compounds.
- -
-
Page/Page column 21
(2011/04/18)
-
- PYRROLIDINE DERIVATIVES
-
The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of pyrrolidine.
- -
-
Page/Page column 26
(2011/09/14)
-
- PYRROLIDINE DERIVATIVES
-
The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of pyrrolidine.
- -
-
Page/Page column 58
(2011/09/14)
-
- Synthesis and Topical Antiinflamatory Activity of Some Steroidal Isoxazolidines
-
1,3-Dipolar cycloaddition of N-methylnitrone, N-benzylnitrone, and pyrroline N-oxide to 1,4,16-pregnatriene-3,20-diones is described.In each case only isoxazolidines were isolated.The pentacyclic adducts 16-19 were active topical antiinflammatory agents in mice, with 18 being more potent than any of the standard compound tested.The hexacyclic adduct 20 was inactive in this assay.
- Green, Michael J.,Tiberi, Robert L.,Friary, Richard,Lutsky, Barry N.,Berkenkoph, Joseph,et al.
-
p. 1492 - 1495
(2007/10/02)
-