446292-10-0Relevant articles and documents
Oxazolidinone derivative and preparation method thereof
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Paragraph 0018; 0020, (2020/03/05)
The invention relates to a preparation method of an oxazolidinone compound impurity 5-chloro-nitrogen-[[(5S)-2-oxo-3-[4-acetamidophenyl]-1, 3- oxazolidine-5-yl]methyl] thiophene-2-methanamide (formulaI) in rivaroxaban. According to a preparation method, 4-aminoacetanilide (formula II) and (S)-N-epoxypropyl phthalimide (formula III) are used as raw materials, and the impurity is obtained through ring opening coupling, ring closing, protecting group removal and condensation reaction. The compound represented by formula I can be applied to rivaroxaban bulk drug quality control and qualitative and quantitative research and detection of impurities.
A [...] synthesis process
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, (2019/01/16)
The invention relates to the technical field of heterocyclic chemistry, specifically to the technical field of nitrogen-oxygen heterocyclic chemistry. Specifically speaking, the invention discloses a novel synthetic process for rivaroxaban. According to the process, the R group of a compound with a structure as shown in a formula (I) is removed so as to obtain a compound with a structure as shown in a formula (II) or an acid salt thereof, and the compound with the structure as shown in the formula (II) or the acid salt thereof reacts with a compound with a structure as shown in a formula (III) under the action of alkali so as to prepare rivaroxaban, wherein the formulas are described in the specification, and R in the formulas is a C1-20 aliphatic/aromatic hydrocarbon group.
Synthesis preparation method of rivaroxaban key intermediate
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Paragraph 0076-0079, (2020/01/03)
The invention discloses a synthesis preparation method of a key intermediate for synthesizing rivaroxaban as shown in formula I. The preparation method comprises the following steps: using compounds as shown in formulae II and III as the initial raw materials, performing condensation and cyclization, hydrolysis, oxidation and reductive amination to obtain the key intermediate for synthesizing rivaroxaban as shown in the formula I. The preparation method has the characteristics of being mild in reaction conditions, simple and convenient in process operation, high in stability and controllability, high in atom utilization ratio, environment-friendly, and low in production cost, is suitable for industrial mass production.