A kind of synthetic method of clindamycin phosphate

Abstract

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.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis, and in particular relates to a synthesis method of clindamycin phosphate. Background technique [0002] Clindamycin phosphate is a broad-spectrum antibiotic and is widely used clinically. It is a semi-synthetic derivative of lincomycin hydrochloride, and its mechanism of action is to inhibit bacterial protein synthesis. Its antibacterial spectrum is the same as that of lincomycin, and it is effective against Gram-positive bacteria such as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus hemolyticus, Streptococcus viridans, Pneumococcus pneumoniae, and Bacillus diphtheria, as well as Peptococcus, Peptostreptococcus, Anaerobic bacteria such as Bacteroides fragilis, Fusobacterium, Eubacterium, and Propionibacterium have antibacterial effects. Clindamycin phosphate has good water solubility and is widely used at home and abroad for its antibacterial properties of high eff...

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Problems solved by technology

However, the phosgene produced by solid phosgene under the decomposition of DMF is highly toxic. There have been many vicious accidents in my country where phosgene leaked from companies using solid phosgene and caused death.

The reason for the leakage lies in the process of preparing the solid phosgene solution. The process used by the manufacturer is to first dissolve the solid phosgene in chloroform in the open field, and after fully dissolving, the trichloromethane dissolved in the solid phosgene The methane solution is transferred to the solvent tank with a solvent pipe and transported to the production workshop, and then the chloroform solution dissolved in solid phosgene is vacuum filtered into the high level tank, and the chloroform solution dissolved in solid phosgene is filtered through the pipeline Add it dropwise into a DMF reactor to form a chlorinated reagent. During the whole process, there are many and frequent material transfers and drops, and the chloroform solution dissolved in solid phosgene is in the state of being heated and wet during the transfer process. It is easy to decompose and produce phosgene, which is easy to cause leakage, cause phosgene volatilization and cause poisoning incidents, and there are great safety hazards in operation

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