A kind of preparation method of 3-morpholinone

A technology of morpholinone and hydroxyacetate, which is applied in the field of preparation of 3-morpholinone, can solve problems such as process safety hazards, difficulty in batch production, and severe reactions, and achieve high purity, less side reactions, and easy-to-obtain raw materials Effect
CN108586377BActive Publication Date: 2019-04-05SHANGHAI KELY BIOPHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI KELY BIOPHARMACEUTICAL CO LTD
Publication Date
2019-04-05

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Abstract

The invention provides a method for preparing 3-morpholone. The method comprises the steps that halogen hydride removing is carried out on 2-halogenated ethylamine hydrohaloate under the condition oforganic solvent existing, an obtained reaction system and 2-glycollic acid ester are mixed and then subjected to amine ester exchange reaction to obtain 2-(2-hydroxyacetamido) halothane; ring closurereaction is carried out on the 2-(2-hydroxyacetamido) halothane under the condition of alkali reagent and organic solvent existing to obtain the 3-morpholone. The method for preparing the 3-morpholonehas the advantages that the technology side reaction is less, the product purification is convenient; the operation is simple, the safety is high, the method is environmentally friendly; raw materials are obtained easily, the price is low; the product yield is high (reaches 75.5%), the purity is high (reaches 99% or above), the method is suitable for the industrialized batch production, and the industrialized prospect is good.
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Description

technical field

[0001] The invention relates to the technical field of preparation of pharmaceutical intermediate raw materials, in particular to a preparation method of 3-morpholinone. Background technique

[0002] Rivaroxaban (Rivaroxaban), the chemical name is 5-chloro-nitrogen-((5S)-2-oxo-3-[-4-(3-oxo-4-morpholinyl)phenyl]-1,3 -Azolidin-5-yl-2-thiophene-carboxamide, trade name Xarelto (Xarelto), is a new type of oral anticoagulant factor Xa drug jointly developed by Bayer AG of Germany and Johnson & Johnson of the United States, 2008 First launched in Canada in 2009, it is mainly used for the prevention and treatment of various thromboembolic diseases, such as the prevention of pulmonary embolism (PE) and deep vein thrombosis (DVT) in adult patients after elective hip or knee replacement. One of the most promising antithrombotic drugs.

[0003] 3-Morpholinone is the key raw material for the preparation of rivaroxaban. At present, 3-morpholinone has the following sever...

Claims

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