Synthesis method of ceftaroline fosamil intermediate

Abstract

The invention provides a method for synthesizing a ceftaroline fosamil intermediate by using a methylation reagent, which is characterized in that in a polar solvent, 7-phenylacetamido-3-[4-(1-methyl-4-pyridine)-2-thiazole sulfydryl]-3-cephem-4-carboxylic acid diphenyl methyl ester reacts with iodized trimethyl sulfinyl sulfonium salt to obtain the ceftaroline fosamil intermediate. The method can solve the problem of potential safety hazards in the prior art, and is simple to operate and high in yield.

Description

A kind of synthetic method of ceftaroline fosamil intermediate technical field The present invention relates to the technical field of drug synthesis, particularly a kind of important synthetic ceftaroline fosamil of methylating reagent Intermediate 7β-amino-3-[4-(1-methyl-4-pyridinium)-2-thiazolylthio]-3-cephem-4-carboxylate benzhydryl iodide matter. Background technique Ceftaroline is the 5th generation cephalosporin antibiotic, is derived from the 4th generation cephalosporin ceftazolam, and is obtained by the Japanese Developed by Ben Takeda Pharmaceutical Co., Ltd., and licensed by Forest Laborstories, Inc., USA, on October 29, 2010 Approved by the U.S. FDA for the treatment of adult community-acquired bacterial enteritis, acute bacterial skin and soft tissue infections infections, including those caused by MRSA. Ceftaroline fosamil is a prodrug of ceftaroline, which increases its stability and will It is rapidly hydrolyzed to ceftaroline and exerts its eff...

AI Technical Summary

Problems solved by technology

This scheme utilizes the trimethylsulfinylsulfonyl iodide salt [(CH 3 ) 3 S + =OI - ] is a relatively easy-to-preserve solid salt with a melting point of 200°C. It has strong methylation ability when applied to the reaction of the present invention, and the characteristics that the reaction can be carried out at room temperature solve the problem of safety in the prior art. Hidden problems

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