556801-12-8Relevant articles and documents
Intermediate for synthesizing rivaroxaban, synthesizing method and application
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Paragraph 0052; 0053; 0054, (2019/01/05)
The invention discloses an intermediate for synthesizing rivaroxaban, a synthesizing method and application. The synthesizing method comprises the following steps: firstly, carrying out addition reaction on a structure of formula II and a structure of formula III to obtain a corresponding amino alcohol compound, and then carrying out cyclization reaction on the amino alcohol compound and a carbonylation reagent to obtain a compound of the structure of formula I; carrying out oxidation reaction on the compound of the structure of formula I and an oxidizing agent to obtain a compound of a structure of known formula IV; secondly, desorbing phthaloyl from the compound of the structure of formula IV according to a known method to obtain a compound of a structure of known formula V; and finally,carrying out acylation reaction on the compound of the structure of formula V to obtain the rivaroxaban (a structure of formula VI). The solvent used in the addition reaction is isopropanol or ethanol, and the addition reaction is carried out at a room temperature or under a heating condition. The intermediate for synthesizing the rivaroxaban, the synthesizing method and the application are designed. The intermediate for synthesizing the rivaroxaban has the advantages of cheap and easily obtained raw materials, gentle and easily operated reaction conditions, environmental protection and lesspollution, high yield and purity, easiness in industrialization and the like.