1252018-07-7

Upstream product

• 2524-67-6 4-morpholino-4-yl-phenylamine 
• 7456-87-3 carbonic acid monomethyl ester 
• 438056-69-0 4-(4-aminophenyl)morpholin-3-one 
• 79-22-1 methyl chloroformate 

Downstream Products

• 366789-02-8 Rivaroxaban 
• 438056-69-0 4-(4-aminophenyl)morpholin-3-one 
• 898543-06-1 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidine-3-yl]phenyl}morpholin-3-one hydrochloride 
• 1414932-73-2 (S)-4-(4-{5-[(benzylidene-amino)-methyl]-2-oxo-oxazolidine-3-yl}-phenyl)-morpholin-3-one 
• 446292-10-0 4-[4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morpholine-3-one 
• 1416129-92-4 tert-butyl {(5S)-3-[4-(3-oxo-4-morpholinyl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methylcarbamate 

Relevant academic research and scientific papers

Preparation method of Rivaroxaban intermediates

The invention discloses a preparation method of Rivaroxaban intermediates. The invention relates to a green and efficient preparation method of 4-(4-aminophenyl)morpholinyl-3-one and an amino protected derivative thereof. A structure of a formula II is obtained through an oxidation reaction of a structure of a formula II, and a structure of a formula I can be obtained through a deprotection reaction of the structure of the formula II, wherein the compound I and the compound II are both important intermediates for synthesizing the anticoagulation drug Rivaroxaban. Potassium permanganate is usedas an oxidizing agent in the oxidation reaction, tetraethyl benzyl ammonium chloride (TEBAC) is used as a phase transfer catalyst, dichloromethane is used as a solvent, and the reaction temperature in the oxidation reaction is 15-55 DEG C. The invention provides the preparation method of the Rivaroxaban intermediates, and the preparation method has the advantages that the raw materials are cheapand easily available, the reactions are mild in condition and are easy to operate, the preparation method is green and is friendly to the environment, the intermediate products and the final product are easy to purify, the total yield is high, industrial production is easy to realize, and the preparation method is effective and practical.

Rivaroxaban synthesis and refining method

The invention discloses a novel rivaroxaban synthesis and refining method. The novel rivaroxaban synthesis and refining method is characterized by adopting new initial raw materials and a refining method thereof. The method disclosed by the invention is simple to operate, stable and reliable in the process, high in product yield and high in optical purity (ee% value), thereby being very suitable for large-scale industrialized rivaroxaban production.

Processes for the preparation of rivaroxaban and intermediates thereof

This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8: