Method for removing protective groups and preparing dimethoxy taxane compound

A technology for dimethoxytaxane and deprotection group, which is applied in the field of preparation of dimethoxytaxane compounds by deprotection group, can solve the problems of reducing reaction yield and product purity, and achieve improvement of reaction yield and product purity, simple operation, and easy industrial production
CN102424672AInactive Publication Date: 2012-04-25JIANGSU HONGDOUSHAN BIOLOGICAL TECH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JIANGSU HONGDOUSHAN BIOLOGICAL TECH
Publication Date
2012-04-25
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a method for removing protective groups and preparing a dimethoxy taxane compound. The invention belongs to the technical field of medicines used for treating prostate cancer. According to the invention, an acid is dissolved in methanol; silica gel with a specification of 100-800 meshes is added to the solution, and the solution is sufficiently stirred under room temperature; the solution is dried by rotary evaporation, such that acid-activated silica gel is obtained; the acid-activated silica gel is dissolved in an organic solvent; a compound 3-Boc-2-p-methoxy phenyl-4-phenyl-(2R,4S,5R)-1,3-oxazolidine-5-carboxylate 4alpha-acetoxy-2alpha-benzoyloxy-5beta,20-epoxy-1beta-hydroxyl-9-oxygen-7beta,10beta-dimethoxy-11-taxadiene-13alpha ester is added to the solution; the mixture is continuously stirred, and is subject to a reaction; an obtained reaction liquid is processed through pump filtration; an obtained filtrate is dried by condensation, and is processed through silica gel column chromatography, such that the product dimethoxy taxane compound is obtained. According to the invention, the protective groups are removed in an acidic environment, such that the dimethoxy taxane compound is prepared. The method is advantaged in simple operation, suitability for industrialized productions, no by-product during the reaction process, improved reaction yield, and improved product purity.
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Description

technical field

[0001] The present invention relates to a method for preparing dimethoxytaxane compounds through deprotection, in particular to a method for preparing dimethoxytaxanes through 3-tert-butoxycarbonyl-2-p-methoxyphenyl-4-phenyl-(2R, 4S,5R)-1,3-oxazolidine-5-carboxylic acid 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-9-oxo-7β,10β- Deprotection of dimethoxy-11-taxene-13α ester to prepare 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy The method of -9-oxotaxane-11-ene-13α-yl-(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxyl-3-phenylpropionate belongs to the drug for treating prostate cancer technology field. Background technique

[0002] 4α-acetoxy-2α-benzoyloxy-5β, 20-epoxy-1β-hydroxy-7β, 10β-dimethoxy-9-oxotaxane-11-en-13α-yl- (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (2) is an effective drug for the treatment of advanced prostate cancer. Patent CN 1179776A discloses a preparation method of this compound, that is, throu...

Claims

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