1349248-79-8

Upstream product

• 1252018-28-2 4-{4-[(5R)-5-(chloromethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one 
• 1325210-64-7 4-(4-isocyanatophenyl)morpholin-3-one 
• 29518-11-4 4-phenylmorpholin-3-one 
• 122-98-5 2-Anilinoethanol 
• 438056-69-0 4-(4-aminophenyl)morpholin-3-one 
• 446292-04-2 4-(4-nitrophenyl)-3-morpholinone 
• 1429334-05-3 4-[4-{(R)-2-hydroxy-3-azidopropylamino}phenyl]morpholin-3-one 
• 105-58-8 Diethyl carbonate 
• 530-62-1 1,1'-carbonyldiimidazole 
• 1313613-18-1 [4-(3-oxo-morpholin-4-yl)phenyl]carbamic acid benzyl ester 
• 681225-50-3 (2S)-1-azido-3-chloropropan-2-ol 
• 1117893-60-3 4-{4-[(5R)-5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one 
• 1424942-80-2 (R)-(2-oxo-3-(4-(3-oxo-morpholino)phenyl)oxazolidin-5-yl)methyl 4-methylbenzene sulfonate 
• 1447919-71-2 4-(4-((R)-5-((phenyloxycarbonyloxy)methyl)-2-oxo-oxazolidin-3-yl)phenyl)-morpholin-3-one 

Downstream Products

• 446292-10-0 4-[4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morpholine-3-one 
• 366789-02-8 Rivaroxaban 

Relevant academic research and scientific papers

Rivaroxaban intermediate preparation method

The invention discloses a rivaroxaban intermediate preparation method. 4-(4-aminophenyl)morpholinyl-3-one and S-glycidol as staring raw materials are synthesized into a compound shown in the structural formula (IV), wherein in the formula (IV), R represents methyl, p-methylphenyl, phenyl or trifluoromethyl. The rivaroxaban intermediate preparation method has the advantages of mild reaction conditions, operation simpleness, high yield and industrialization easiness.

PROCESS FOR PREPARATION OF OXAZOLIDINONE DERIVATIVES

A process for preparation of oxazolidinone derivatives such as Linezolid and Rivaroxaban using (S)-Epichlorohydrin.

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

The present invention relates to processes for the preparation of oxazolidinone derivatives. More particularly the present invention provides processes for the preparation of 5-chloro-N-( {(5S)-2-oxo-3-[4-(3-oxo-4-moφholinyl)phenyl]-1,3-oxazolidin-5-yl methyl)-2-thiophene-carboxamide and intennediates thereof. Where L is a leaving group like halogen atom (F, CI, Br, I) or -OS02R where R = C'-4 alkyl straight chain or branched chain, sub or unsubstituted aryl, sub or unsub aryl alkyl; with a suitable reagent to provide the compound of formula (II). The reaction step is performed by reacting the compound of formula (IV) with amine source which may be dissolved in solvent like water or alcohol. For example ammonium hydroxide.

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.

PROCESSES FOR THE PREPARATION OF 4-{4-[5(S)-(AMINOMETHYL)-2-OXO-1,3-OXAZOLIDIN-3-YL]PHENYL} MORPHOLIN-3-ONE

The present invention provides simple, eco-friendly, cost-effective, reproducible, robust and industrial processes for the preparation of intermediate compound 4-{4-[5(S)-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one (II). The present invention also provides novel intermediates and their use in the synthesis of morpholinone oxazolidine derivatives.

An approach to the anticoagulant agent rivaroxaban via an isocyanate-oxirane cycloaddition promoted by MgI2.etherate

A convergent and efficient synthesis of anticoagulant rivaroxaban was developed using the cycloaddition of commercially available (R)-epichlorohydrin with 4-(morpholin-3-one)phenyl isocyanate catalysed by MgI2 etherate as the key step, in 22% overall yield.