Method for synthesizing rivaroxaban intermediate 4-(4-aminophenyl)-3-molindone

A technology of aminophenyl and rivaroxaban, which is applied in the field of medicine, can solve problems such as low product yield, serious environmental pollution, and harsh reaction conditions, and achieve simple synthesis operation, reduced environmental pollution, and high total yield Effect
CN103524447AActive Publication Date: 2014-01-22SHANDONG BOYUAN PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG BOYUAN PHARM CO LTD
Publication Date
2014-01-22

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Abstract

The invention discloses a method for synthesizing a rivaroxaban intermediate 4-(4-aminophenyl)-3-molindone. The method comprises the following steps: reacting paranitroaniline with ethylene oxide to obtain a compound II; performing a cyclization reaction on the compound II and bromoacetyl bromide to obtain a compound III; adding the compound III into iron powder to perform a reduction reaction to obtain the 4-(4-aminophenyl)-3-molindone. According to the method, the raw materials are low in cost and easily obtained, the cost is low, the synthesis operation is simple, industrial nitration is avoided, environmental pollution is greatly reduced, and the method is suitable for industrial production.
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Description

technical field

[0001] The invention relates to a method for synthesizing 4-(4-aminophenyl)-3-morpholinone, an intermediate of rivaroxaban, and belongs to the technical field of medicine. Background technique

[0002] Rivaroxaban is a well-established anticoagulant mainly used to prevent the formation of deep vein thrombosis (DVT) and pulmonary embolism (PE) in patients after hip and knee arthroplasty. It can also be used to prevent stroke and non-central nervous system embolism in patients with non-valvular atrial fibrillation, and reduce the risk of coronary syndrome recurrence. Rivaroxaban highly selectively and competitively inhibits free and bound factor Xa and prothrombin activity, prolonging the activated partial thromboplastin time plate (PT) and prothrombin time (aPTT) in a dose-dependent manner. The essential difference between rivaroxaban and fondaparinux / heparin is that it does not require the participation of antithrombin III and can directly antagonize free an...

Claims

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