Refining process of tedizolid and preparation method of tedizolid phosphate

Abstract

The invention belongs to the field of medicine synthesis, and discloses a refining process of tedizolid. According to the invention, a mixed solution of dichloromethane, toluene and ethanol is prepared, tedizolid generated through Suzuki reaction is purified through steps of liquid separation, filtration and the like, and the obtained tedizolid pure product is used for tedizolid phosphate synthesis. While the purity of tedizolid is ensured, the consumption of tedizolid in the refining process is reduced, the yield of tedizolid is improved, the utilization rate of raw materials is improved, the production cost is saved, the tedizolid with higher purity participates in synthesis of tedizolid phosphate, the side reaction in the tedizolid phosphate synthesis process is reduced, the purification difficulty of tedizolid phosphate is reduced, and the purity and the yield of tedizolid phosphate are improved. The method is suitable for refining tedizolid compounds, and is especially suitable for refining an intermediate tedizolid in a tedizolid phosphate synthesis process.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and relates to a refining process for synthesizing an intermediate of tedizolid phosphate, in particular to a refining process for tedizolid. Background technique [0002] Tedizolid phosphate was approved by the US FDA in 2014 for complicated skin and soft tissue infections caused by methicillin-resistant aureus. Tedizolid Phosphate is a bacterial protein synthesis inhibitor and an upgraded version of Linezolid. Different from traditional antibiotics, tedizolid phosphate selectively binds to bacterial 50S subunit ribosomes, interferes with the formation of 70S initiation complexes including mRNA, 30S ribosomes and initiation factors, thereby inhibiting bacterial protein synthesis. Because this inhibition process is in the early stage of protein translation, it is not easy to cross-resistance to antibiotics with other mechanisms. [0003] There are many patents disclosing the synthetic method of te...

AI Technical Summary

Problems solved by technology

[0005] Among them, there have been a lot of reports on the purification and purification of tedizolid phosphate, but there is little mention of the purification and purification of its intermediate tedizolid, but the purity and yield of tedizolid are higher than that of tedizolid phosphate. The synthesis of amines has a very important influence. The purity of tedizolid is not enough and contains too many impurities. In the process of synthesizing tedizolid phosphate, the impurities and phosphorus oxychloride will take the lead in side reactions, resulting in the formation of new impurities and Inhibit the synthesis of tedizolid phosphate, reduce the yield of tedizolid phosphate and increase the difficulty of subsequent purification; at the same time, the yield of tedizolid phosphate is not high, which will naturally lead to the reduction of tedizolid phosphate yield, using a large amount of However, a small amount of products are obtained, and the palladium catalyst used in the synthesis is very expensive, which undoubtedly increases the production cost and increases the production burden of the enterprise. Therefore, a refining process is needed to ensure the purity of tedizolid Simultaneously improve the yield for the synthesis of tedizolid phosphate

Images