Synthetic method of doxylamine succinate

A technique for the synthesis of doxylamine succinate, which is applied in the fields of medical technology and organic synthesis, can solve the problems of low melting point, insufficient purity, and toxic benzene by-products, and achieve safe and reliable processes, simple post-processing, and easy raw materials. The effect
CN107056685AInactive Publication Date: 2017-08-18珠海市海瑞德生物科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
珠海市海瑞德生物科技有限公司
Publication Date
2017-08-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthetic method of doxylamine succinate. The synthetic method specifically comprises the following three reaction steps: (1) synthesizing 2-pyridylphenyl methyl methanol from acetophenone and 2-bromopyridine in the presence of butyl lithium; (2) reacting by virtue of 2-pyridylphenyl methyl methanol with 2-dimethylamino chloroethane under the action of organic alkali so as to generate doxylamine free alkali; and (3) carrying out salt formation reaction by virtue of doxylamine free alkali and succinic acid, so as to generate doxylamine succinate. The synthetic method has the beneficial effects that the raw materials are easily available, the yield is high, the cost is low, an acceptable product can be obtained without carrying out chromatographic column separation on the product of each step, the process is simple, the post-treatment is simple, the process is safe and reliable, and the synthetic method is suitable for large-scale production.
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Description

technical field

[0001] The invention belongs to the technical fields of medical technology and organic synthesis, and in particular relates to a synthesis method of doxylamine succinate, an ethanolamine antihistamine. Background technique

[0002] Doxylamine succinate is a kind of ethanolamine drug, which has antihistamine effect, anticholinergic effect and significant sedative effect. It has strong activity and low gastrointestinal side effects, and is suitable for a variety of allergic skin diseases. Hay fever, allergic rhinitis, asthmatic bronchitis, etc., doxylamine succinate is a non-psychotropic, non-regulated over-the-counter drug. In October 1978, the FDA approved the marketing of doxylamine 25mg tablets from CHATTEM, which is used to help Relieve difficulty in falling asleep, became OTC in 1979, approved in September 1996 and approved the listing of generic drugs of LNK Company in August 2004. On April 8, 2013, the FDA approved Diclegis (doxylamine succinate and py...

Claims

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