1354900-66-5Relevant articles and documents
Preparation method of cabazitaxel
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, (2021/11/27)
The invention discloses a preparation method of cabazitaxel, which comprises the following specific steps: dissolving 10-deacetylbaccatin III with dichloromethane and pyridine, dropwise adding 2,2,2-trichloroethyl chloroformate, and treating to obtain an intermediate I; mixing toluene, 4-dimethylaminopyridine, the intermediate I and (4S,5R)-3-tert-butoxycarbony-2-(4-anisy)- 4-phenyl-5-oxazolidinecarboxylic acid, stirring, dropwise adding N,N'-dicyclohexylcarbodiimide, and stirring for reaction to obtain an intermediate II; dissolving the intermediate II with ethyl acetate and acetic acid, adding zinc powder, carrying out a stirring reaction to obtain an intermediate III, dissolving the intermediate III with dichloromethane, adding 1,8-bis(dimethylamino)naphthalene, a molecular sieve and trimethyloxonium tetrafluoroborate, and carrying out a stirring reaction to obtain an intermediate IV; dissolving and clarifying the intermediate IV with methanol, dropwise adding a hydrochloric acid methanol solution having a concentration of 1mol/L, and stirring for reaction to obtain cabazitaxel. According to the method, methylation can be realized at room temperature, the product purity is good, the yield is high, starting materials are easy to obtain, and large-scale preparation can be carried out.
Kaba he of the intermediate compounds (by machine translation)
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Paragraph 0171 - 0173, (2017/05/25)
The present invention relates to intermediate compounds of Kabbah, in particular for the preparation of the intermediate compound he Kabbah 6, preparation method thereof, and he Kabbah for preparing the compound of the method. Intermediates to of the present invention the process of preparing kaba he races, in each step of the reaction time is greatly shortened, the reaction yield is greatly improved, greatly reduces the cost of synthesizing of Kabbah. (by machine translation)