99570-29-3Relevant academic research and scientific papers
Epirubicin hydrochloride than star-intermediate compound (by machine translation)
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, (2017/07/21)
The present invention provides novel intermediates and utilizing the intermediate synthesis than the star of epirubicin hydrochloride new routes. The route is simple, low-cost, high-efficiency, at the same time avoiding the existing epirubicin hydrochloride than star-synthetic route to produce the intermediate with water not stable, easily decomposed, the overall line rate is on the low side, in order to better energy-saving and emission reduction, the routes using low cost and easily obtained reagent; at the same time adopts the removable selective protection means, produce little impurity, high purity, high yield. (by machine translation)
SYNTHESIS OF EPIRUBICIN FROM 13-DIHYDRODAUNORUBICINE
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Page/Page column 6, (2008/06/13)
A method of preparing an anthracyclin such as epirubicin from a starting material comprising 13-dihydrodaunorubicine (13-daunorubicinol). The method comprises producing N-Trifluoroacetyl-13-daunorubicinol from 13-daunorubicinol by acylation. The N-Trifluoroacetyl-13-daunorubicinol is reacted with an aprotic solvent and an acylating agent to produce an intermediate sulfoxy salt which is treated with a strong base to produce 4′-keto-N-Trifluoroacetyldaunorubicin. The 4′-keto-N-Trifluoroacetyldaunorubicin is reacted with a reducing agent, such as borohydride of an alkaline metal, to produce N-Trifluoroacetyl-4′-epi-daunorubicin. The N-Trifluoroacetyl-4′-epi-daunorubicin is hydrolyzed in a basic solution to produce an intermediate compound. The intermediate compound is reacted with a halogenizing agent to produce a 14-Hal-derivative. The 14-Hal derivative is hydrolized in the presence of a formate of an alkaline metal to produce the desired final compound.
