1416129-92-4

Upstream product

• 1325210-64-7 4-(4-isocyanatophenyl)morpholin-3-one 
• 161513-47-9 (S)-<<(tert-butoxycarbonyl)amino>methyl>oxirane 
• 415684-05-8 tert-butyl (2S)-3-chloro-2-hydroxypropylcarbamate 
• 635301-86-9 [4-(3-oxo-morpholin-4-yl)-phenyl]-carbamic acid 4-nitro-phenyl ester 
• 1252018-07-7 methyl N-[4-(3-oxo-4-morpholinyl)phenyl]carbamate 
• 1313613-18-1 [4-(3-oxo-morpholin-4-yl)phenyl]carbamic acid benzyl ester 
• 415684-06-9 (1S)-2-[(tert-butoxycarbonyl)amino]-1-(chloromethyl)ethyl acetate 
• 1429333-95-8 tert-butyl N-[(R)-2-hydroxy-3-{4-(3-oxomorpholin-4-yl)phenylamino}propyl]carbamate 
• 530-62-1 1,1'-carbonyldiimidazole 
• 438056-69-0 4-(4-aminophenyl)morpholin-3-one 
• 1429333-94-7 tert-butyl (2S)-3-chloro-2-((phenyloxycarbonyl)oxy)propylcarbamate 

Downstream Products

• 366789-02-8 Rivaroxaban 
• 898543-06-1 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidine-3-yl]phenyl}morpholin-3-one hydrochloride 
• 446292-10-0 4-[4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morpholine-3-one 

Relevant academic research and scientific papers

A [...] synthesis process

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.

NOVEL METHOD FOR SYNTHESIZING RIVAROXABAN INTERMEDIATE, 4-MORPHOLIN-3-ONE

The present invention discloses novel methods for synthesizing Rivaroxaban intermediate, i.e., 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3 -oxazolidin-3 -yl]phenyl}morpholin-3-one. The novel methods provided in the present invention involve mild reaction conditions, convenient operations, easy purification, and low production costs, and thus the process is environmental-friendly and suitable for industrial production.

NOVEL METHOD FOR SYNTHESIZING RIVAROXABAN INTERMEDIATE, 4-{4-[(5S)-5-(AMINOMETHYL)-2-OXO-1,3-OXAZOLIGDIN-3-YL]PHENYL}MORPHOLIN-3-ONE

The present invention discloses novel methods for synthesizing Rivaroxaban intermediate, i.e., 4- {4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl} morpholin-3-one. The novel methods provided in the present invention involve mild reaction conditions, convenient operations, easy purification, and low production costs, and thus the process is environmental-friendly and suitable for industrial production.

PROCESSES FOR THE PREPARATION OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(3-OXO-4-MORPHOLINYL) PHENYL]-1,3-OXAZOLIDIN-5-YL}METHYL)-2-THIOPHENE-CARBOXAMIDE AND INTERMEDIATES THEREOF

TThe present invention provides processes for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide (I) and intermediates thereof. Also provides novel intermediates and their use in the synthesis of oxazolidine derivatives.