- Synthesis method of clindamycin phosphate and application
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The invention belongs to the field of medicine synthesis, and discloses a synthesis method of clindamycin phosphate. The method comprises the following steps: chloridizing tert-butyl (2-chloro-1-(3,4,5-trihydroxy-6-(methylthio) tetrahydro-2H-pyran-2-yl) propyl) carbamate with phosphorus trichloride, esterifying with phosphorus oxychloride, and finally carrying out condensation reaction with 1-methyl-4-propyl pyrrolidine-2-carboxylic acid, so as to obtain the clindamycin phosphate. According to the synthesis method of clindamycin phosphate, molecules with small molecular weight are used as raw materials, so that the purification difficulty of an intermediate is reduced, the recovery rate of the intermediate is improved, and the production cost is reduced. The invention also provides an application of the synthesis method of the clindamycin phosphate, the synthesis method is used for synthesizing the clindamycin phosphate, and the obtained clindamycin phosphate is used for preparing the clindamycin phosphate injection.
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Paragraph 0023; 0029-0030; 0031-0038
(2021/07/17)
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- Clindamycin phosphate preparation method
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The invention discloses a clindamycin phosphate preparation method. The method sequentially includes steps: adopting clindamycin 3,4-isopropylidene as a raw material, performing reaction with dibenzoxycarbonyl phosphoryl chloride, hydrogenating to remove a benzyl protection group, and finally hydrolyzing under an acidic condition to obtain a product of clindamycin phosphate. Extensive and sufficient material sources, low cost, mild reaction conditions and simple process are realized, each reaction step is conventional in operation, difficulty in purification due to adoption of low-selectivityphosphorus oxychloride is avoided, and a wide application range is realized.
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Paragraph 0015; 0019; 0021
(2018/12/02)
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- Preparation method of clindamycin phosphate
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The invention belongs to the technical field of chemical synthesis and relates to a preparation method of clindamycin phosphate. The preparation method includes preparing clindamycin isopropylidene alkali from clindamycin hydrochloride monohydrate, subjecting the clindamycin isopropylidene alkali to phosphate esterification with phosphorus oxychloride as a phosphate esterification agent and 1,2,4-triazole as an acid-binding agent to obtain isopropylidene clindamycin phosphate, and subjecting the isopropylidene clindamycin phosphate to deprotection by hydrolysis of mixed acid to obtain the clindamycin phosphate. The preparation method has the advantages that by preparing the clindamycin phosphate through one-step hydrolysis of organic acid, the preparation method is energy saving and environment friendly; the preparation method is high in yield and low in cost and can obtain the high-purity finished product directly without subsequent refining, so that the molar yield of the clindamycinphosphate can reach 96.15%; the clindamycin phosphate is good in crystal form (bulk density and liquidity), so that aseptic packaging is benefited.
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Paragraph 0051; 0056-0057; 0063-0064; 0070-0071
(2018/03/26)
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- Triazole in the synthesis of clindamycin phosphate in the application of the
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The invention relates to an application of tolyltriazole in clindamycin phosphate synthesis. According to the application, pyridine and triethylamine are replaced by the tolyltriazole, so that the tolyltriazole, phosphorus oxychloride and a compound in a first formula can perform phosphate esterification reaction in solvent to obtain a solution of a compound in a second formula. A method for synthesizing the clindamycin phosphate is more efficient, low in cost, economical in energy and environmentally friendly due to the application of the tolyltriazole, and the obtained clindamycin phosphate is high in yield and purity.
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Paragraph 0015; 0025-0026
(2017/11/16)
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- A clindamycin phosphate ester synthesis method
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The invention belongs to the technical field of chemical synthesis and specifically relates to a synthetic method of clindamycin phosphate. The method comprises the following steps of synthesis of clindamycin free alkali, ketonization reaction, phosphorylation reaction and aftertreatment. According to the invention, the weight yield of the clindamycin phosphate can reach over 80% by changing a charging sequence, steps and a catalyst.
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Paragraph 0042; 0045-0046
(2017/02/28)
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- Clindamycin-2-phosphoryl benzylate
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A novel compound, also known as 7(s)-chloro-7-deoxylincomycin-2-phosphoryl benzylate, useful an an intermediate in the production of the antibiotic, clindamycin-2-phosphate.
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