Preparation method of rivaroxaban intermediate

Preparation method of rivaroxaban intermediate

The invention discloses a preparation method of a rivaroxaban intermediate, (S)-2-((3-(4-morpholinophenyl)-2-oxazolidin-5-yl) methyl) isoindoline-1, 3-dione (II) is taken as a starting material, sodium chlorite is taken as an oxidizing agent, the rivaroxaban intermediate (I) is obtained through oxid...

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Hauptverfasser: SUN BINGFENG, ZHU CHENLONG, LI NANLIAN, XU HONGYU, LIN XIAOYU, SON BYUNG-JUN
Format: Patent
Sprache:chi ; eng
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator SUN BINGFENG
ZHU CHENLONG
LI NANLIAN
XU HONGYU
LIN XIAOYU
SON BYUNG-JUN
description The invention discloses a preparation method of a rivaroxaban intermediate, (S)-2-((3-(4-morpholinophenyl)-2-oxazolidin-5-yl) methyl) isoindoline-1, 3-dione (II) is taken as a starting material, sodium chlorite is taken as an oxidizing agent, the rivaroxaban intermediate (I) is obtained through oxidation reaction, and the reaction route is shown in the specification. The preparation method specifically comprises the following steps: S1, carrying out addition reaction on a compound (II) and a compound (III) to obtain a corresponding amino alcohol compound, and carrying out cyclization reaction on the amino alcohol compound and a carbonylation reagent to obtain a compound (IV); s2, dissolving the compound (IV) in a polar aprotic solvent, and adding an oxidizing agent and an auxiliary reagent for reaction to obtain a reaction solution; and S3, concentrating, washing and drying the reaction liquid to obtain a crude product, and purifying the crude product through column chromatography or recrystallization to obta
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title Preparation method of rivaroxaban intermediate
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