1372665-04-7Relevant articles and documents
A method for the preparation of key intermediate the advantage cuts down Sha Ban
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, (2017/08/25)
The invention relates to a preparation method of a rivaroxaban key intermediate, particularly a preparation method of 4-[4-[(5S)-5-(aminomethyl)-2-oxo-3-oxazolidinyl]phenyl]-3-morpholone hydrochloride (compound 4), which comprises the following steps: reacting dibenzyl ammonia with R-epoxy chloropropane to obtain N,N-dibenzyl epoxypropane (compound 1), reacting the compound 1 with 4-(4-aminophenyl)morpholinyl-3-one to obtain a compound 2, reacting the compound 2 with N,N-carbonyl-diimidazole to obtain a compound 3, and catalyzing the compound 3 with palladium on carbon to obtain the 4-[4-[(5S)-5-(aminomethyl)-2-oxo-3-oxazolidinyl]phenyl]-3-morpholone hydrochloride.
METHOD FOR PREPARING RIVAROXABAN INTERMEDIATE
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Paragraph 0028; 0040; 0041, (2015/03/03)
Disclosed is a method for preparing a Rivaroxaban intermediate I, comprising the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C to 60° C, where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to 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
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, (2013/07/25)
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.