Synthesis method of doxylamine succinate

A technology of doxylamine succinate and synthesis method, which is applied in the field of synthesis of doxylamine succinate, can solve the problems of reaction equipment damage, long reaction time, and high cost of doxylamine, and achieve anticholinergic sedation effect, low gastrointestinal side effects, significant sedative effect
CN110498764APending Publication Date: 2019-11-26深圳沃兰德药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
深圳沃兰德药业有限公司
Publication Date
2019-11-26

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Abstract

The invention discloses a synthesis method of doxylamine succinate. The method includes: (1) adding 2-pyridylphenylmethylcarbinol into an organic solvent I, adding a catalyst, strong base or alkali metal and 2-dimethylaminochloroethane respectively, performing heating to 100-110DEG C and carrying out reaction for 1-2h; then conducting cooling and filtering; subjecting an aqueous phase to backwashing with the organic solvent I, then performing heating to 70-80DEG C, adding activated carbon for decolorization, then performing filtering, then adding a low-boiling-point organic solvent for extraction, drying the extracted organic phase, and finally conducting reduced pressure concentration at 50-60DEG C to dryness to obtain doxylamine; and (2) dissolving the doxylamine in an organic solvent II, adding succinic acid at 50-60DEG C for reaction, then employing medicinal activated carbon for decolorization and filtering, conducting cooling to a temperature at or below 5DEG C, carrying out stirring crystallization, then performing pumping filtering, and conducting washing with the precooled organic solvent II, and finally performing vacuum drying to obtain the doxylamine succinate. The synthesis method provided by the invention simplifies operation, lowers energy consumption, and has high reaction conversion rate and high yield.
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Description

technical field

[0001] The invention relates to the technical field of organic synthesis, in particular to a synthesis technology of doxylamine succinate. Background technique

[0002] Doxylamine succinate is a kind of ethanolamine drug, which has antihistamine effect, anticholinergic effect and significant sedative effect. It has the characteristics of strong activity and low gastrointestinal side effects, and is suitable for a variety of allergic skin diseases. Hay fever, allergic rhinitis, asthmatic bronchitis, etc. The route of synthesizing doxylamine succinate in the existing published patent literature is as follows:

[0003] 2-Pyridylphenylmethylmethanol and 2-dimethylaminoethyl chloride generate doxylamine base under the action of an organic base; then doxylamine base and succinic acid are salified to obtain doxylamine succinate.

[0004] The synthesis method of doxylamine disclosed in patent CN102108059B: 2-pyridylphenylmethylmethanol is reacted with sodium amide ...

Claims

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