- Expeditious synthesis and preliminary antimicrobial activity of deflazacort and its precursors
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The synthesis of deflazacort (DFZ) and a preliminary evaluation of its microbial activity against the human pathogens Acinetobacter baumannii and Staphylococcus aureus is herein reported. While DFZ is inactive, one of its synthetic precursors showed a strong antibacterial activity against both Gram-negative and -positive bacteria.
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- Preparation method of deflazacort
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The present invention relates to a preparation method of deflazacort. The deflazacort is prepared through the following thirteen chemical synthesis reactions of elimination, cyanohydrintion, silanization, translocation and esterification, elimination, epoxidation, protection, ammoniation, cyclization, hydrolysis, bromo hydroxylation, debromination, esterification and the like. Raw materials for the preparation method of deflazacort are easily obtained. Meanwhile, the preparation method of deflazacort is mild in reaction condition, simple in process route and low in pollution, thus having a good application prospect.
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- New process for reducing steroid 11-ketone group
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The invention discloses a method for preparing a steroid 11 beta-hydroxyl compound by reducing a steroid 11-ketone group compound. The method comprises that the steroid 11-ketone group compound and a reduction agent are subjected to a reaction in a non-ester solvent to obtain the steroid 11 beta-hydroxyl compound; the reduction agent is selected from one or more of sodium borohydride, potassium borohydride and lithium borohydride; a metal salt is also added in the reaction system and is selected from one or more of a divalent calcium salt, a divalent magnesium salt, a divalent zinc salt, a divalent copper salt, a divalent cobalt salt, a divalent chromium salt, a tetravalent titanium salt and a trivalent cerium salt; the non-ester solvent is a protic solvent or a mixed solvent of other non-ester organic solvents and the protic solvent. The method has the greatest advantages that the high-purity 11 beta-hydroxyl compound is obtained with high yield at room temperature, and the method is simple in operation, good in repeatability, and easy to industrialize.
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Paragraph 0117; 0118; 0119; 0120; 0121; 0122
(2016/10/09)
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- Method for reducing or preventing transplant rejection in the eye and intraocular implants for use therefor
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Methods for reducing or preventing transplant rejection in the eye of an individual are described, comprising: a) performing an ocular transplant procedure; and b) implanting in the eye a bioerodible drug delivery system comprising an immunosuppressive agent and a bioerodible polymer.
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- Preparation of (11 beta ,16 beta )-21-(acetyloxy)-11-hydroxy-2'-methyl-5'H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione
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PCT No. PCT/EP96/05390 Sec. 371 Date Jun. 5, 1998 Sec. 102(e) Date Jun. 5, 1998 PCT Filed Dec. 4, 1996 PCT Pub. No. WO97/21722 PCT Pub. Date Jun. 19, 1997A process for preparing the compound (11 beta ,16 beta )-21-(acetyloxy)-11-hydroxy-2'-methyl-5'H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione (INN deflazacort) which comprises reacting (11 beta ,16 beta )-11,21 -dihydroxy-2'-methyl-5'H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione with acetic anhydride in a suitable organic solvent in the presence of a basic catalyst and water.
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- Process for the preparation of pregneno-oxazolines
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A process for preparing 11-beta-hydroxy-1,4-pregna-dieno-oxazolines from 4-pregneno-oxazolines in the presence of a sequentially growing mixed culture of a Curvularia strain and an Arthrobacter strain.
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