A kind of synthetic method of S-glycidyl phthalimide

A technology of glycerol phthalimide and potassium phthalimide, applied in the field of medicine and biochemical industry, can solve problems such as unfavorable industrialized production, long reaction time, difficult aftertreatment, etc., and the reaction temperature is not harsh , the effect of high reaction yield and purity, and low production cost
CN109384773BActive Publication Date: 2020-07-17XINFA PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
XINFA PHARMA
Publication Date
2020-07-17

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Abstract

The invention relates to a low-cost and high-purity S-glycidyl phthalimide synthesis method, which comprises: carrying out a substitution reaction on potassium phthalimide and R-2,2-disubstituted-4-halomethyl-1,3-dioxolane to generate N-(S-2,2-disubstituted-1,3-dioxolane-4-)methylphthalimide, carrying out a ketone (aldehyde) removing ring-opening reaction to produce N-2-S-hydroxy-3-halogenated n-propyl phthalimide, and finally carrying out an elimination reaction to remove hydrogen halide so as to generate S-glycidyl phthalimide, wherein S-glycidyl phthalimide is the key intermediate for the preparation of rivaroxaban. According to the present invention, the synthesis method has advantages of inexpensive and easily-available raw materials, high stability, high reaction selectivity and highproduction efficiency, and the obtained S-glycidyl phthalimide has advantages of low cost and high purity, and is favorable for the industrial production of high-purity rivaroxaban.
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Description

technical field

[0001] The invention relates to a method for synthesizing S-glycidyl phthalimide, which belongs to the field of pharmaceutical biochemical industry. Background technique

[0002] Rivaroxaban, known in English as Rivaroxaban, is a new oral anticoagulant drug that is absorbed orally and has a long-lasting effect. It is used to prevent and treat venous thrombosis. It has a wide therapeutic range and does not require routine coagulation function monitoring. The world's first direct factor Xa inhibitor developed for Bayer was approved by the US Food and Drug Administration (FDA) in 2011. Clinically, it is mainly used to prevent the formation of deep vein thrombosis and pulmonary thrombosis in patients after hip and knee replacement. It can also prevent stroke and non-central nervous system embolism in patients with non-valvular atrial fibrillation, and reduce the recurrence of coronary artery syndrome. risk. Its market sales from 2011 to 2016 reached US$5.56 bil...

Claims

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