Optimum Of Synthesis Of Clindamycin Phosphate

This paper introduces the pharmic trait of antibiotic clindamycin hydrochlorid and clindamycin phosphate and discusses the development of their synthesis. The whole reaction route was designed too. The clindamycin phosphate was obtained with 62.7% total yield after 7-hydroxyl of lincomycin hydrochlorid was chlorinated, 3,4-hydroxyl of clindamycin hydrochlorid was protected, osphorylated and hydrolyzed.Clindamycin hydrochlorid can be prepared by the direct chlorination reaction of the Vilsmeier reagent and lincomycin hydrochlorid. After that, the reaction solution was basified, concentrated and alcoholized. The yield reached 88%.Clindamycin 3,4-isopropylidene was synthesized by Clindamycin Hydrochloride at room temperature. During the reaction, acetone was used as a solvent and also a hydroxyl protection reagent to protect 3,4-hydroxyl. After the experiment was repeated for a few times, the optimum reaction condition including temperature, reactant molar ratio and alkaline reagent in the later treatment was fixed. The yield reached 80%.Clindamycin phosphate was successfully prepared by the acylation and hydrolysis reaction of Clindamycin 3,4-isopropylidene. Dilxane was used as solvent in stead of pyridine, and meanwhile, certain amount of pyridine was used as catalyst. The yield reached 88%.In our work, the products were characterized by FT-IR and 1H NMR. The measure methods and research methodology of making sure the content of clindamycin hydrochlorid, clindamycin phosphate and related substance was set up. Clindamycin phosphate with the yield of 62.7% was obtained by following the expected reaction route.