1329837-80-0Relevant articles and documents
Deuterated Rivaroxaban and preparation method thereof
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, (2018/04/21)
The invention discloses deuterated Rivaroxaban, which has a structure shown as a formula (I) in the description. The invention also discloses a preparation method of the deuterated Rivaroxaban. The method comprises the following steps of (1) performing condensation reaction on deuterated-4-p-aminophenyl morpholine-3-ketone and (S)-N-glycidol o-phthalimide; performing filtering; then, washing filter cake; performing reduced pressure drying to obtain a deuteration compound; (2) performing ring-closure reaction on the deuterated compound and N,N'-carbonyldiazole; performing reduced pressure concentration to the dry state; performing washing and filtering; then, performing reduced pressure drying on the filter cake to obtain a second deuterated compound; (3) performing hydrolysis reaction on the second deuterated compound and methylamine ethanol solution; performing concentration to the dry state; then, performing recrystallization by methyl alcohol; performing reduced pressure drying to athird deuterated compound; (4) performing condensation reaction on the third deuterated compound and 5-chloro-2-acyl chloride thiofuran; washing the filter cake after the filtering; performing reduced pressure drying on the filter cake to obtain the Deuterated Rivaroxaban. The deuteration Rivaroxaban has the advantages that the raw materials can be easily obtained; the operation is simple and convenient; the yield is high; deuterium in the initial raw materials is remained to the final product.
