Preparation method of Rivaroxaban intermediate

The invention discloses a preparation method of a Rivaroxaban intermediate. The preparation method includes the following steps that (1) in existence of an organic lithium salt or the organic lithiumsalt and an inorganic lithium salt, a compound in a following formula I is reacted with a compound in...

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Main Authors LI HONGMING, LIANG CHAO, JIANG JUN, QIU ZHIHAI, WU XIAOSHU, ZHU CAN, CHU CHANGHU
Format Patent
LanguageChinese
English
Published 10.12.2019
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention discloses a preparation method of a Rivaroxaban intermediate. The preparation method includes the following steps that (1) in existence of an organic lithium salt or the organic lithiumsalt and an inorganic lithium salt, a compound in a following formula I is reacted with a compound in a following formula II to obtain a compound in a following formula III; and (2) the compound in the formula III is subjected to an acidification reaction in existence of inorganic acid HX, the Rivaroxaban intermediate shown in a following formula IV is obtained, wherein R in the compound in the formula I is selected from methyl, isopropyl, normal-butyl and phenyl or benzyl, and the inorganic acid HX is selected from hydrochloric acid or sulfuric acid. The preparation method is easy to operateand high in yield, and industrial production and patent medicine quality control are convenient. 本发明公开了一种利伐沙班中间体的制备方法，包括如下步骤：(1)在有机锂盐或有机锂盐和无机锂盐的存在下，如下式Ⅰ化合物和如下式Ⅱ化合物反应，得到如下式Ⅲ化合物；(2)将所述的式Ⅲ化合物在无机酸HX存在下进行酸化反应，得到如下式Ⅳ所示的利伐沙班中间体；其中，式Ⅰ
Bibliography:Application Number: CN201910809999