Preparation method of pramoxine hydrochloride
A technology for pramoxaine hydrochloride and hydrochloric acid is applied in the field of preparation of pramoxaine hydrochloride, which can solve the problems of low purity, high price, high production cost, industrialized production and the like, avoid environmental pollution problems, simple and convenient operation, The effect of reducing production costs
Active Publication Date: 2014-04-23
山东诚汇双达药业有限公司
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Problems solved by technology
This reaction must have a chlorination step, the preparation step is longer, the production cost is higher, and the production efficiency is low
Thionyl chloride is used in chlorination, which produces strong irritating gases-hydrogen chloride and sulfur dioxide. These exhaust gases seriously pollute the environment, and pollution control requires high production costs, which is not conducive to large-scale industrial production.
And, the pramoxine hydrochloride purity of preparation is about 98%, and purity is not high
Due to high production costs and small-scale industrial production, this drug is expensive and cannot meet the needs of modern medicine, so all countries are studying the production method of this local anesthetic
Method used
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Experimental program
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Embodiment Construction
[0009] A kind of preparation method of pramoxine hydrochloride of the present invention comprises the following steps:
[0010] ① Dissolve strong base and weak acid salt in water to form a weak alkaline solution; add morpholine and 1-bromo-3-chloropropane to the weak alkaline solution, stir for 30-40 minutes, and then set the temperature at 55-65 °C React at constant temperature in a hot water bath for 4-6 hours, then turn on a cold water bath to cool down to room temperature, let stand at room temperature and separate layers, take the upper layer of oil for rectification, and obtain the intermediate N-(3-chloropropyl)morpholine, morphine The weight ratio of morphine, 1-bromo-3-chloropropane and strong base to weak acid salt is 1:1.57-2.0:0.52-1.27;
[0011] ②Put absolute ethanol and sodium hydroxide into the reaction kettle, stir to dissolve, then add 4-butoxyphenol and N-(3-chloropropyl)morpholine into the reaction kettle, heat up and reflux for 24-26h, and drop to After fi...
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The invention relates to a preparation method of pramoxine hydrochloride. The preparation method comprises the following steps of: dissolving salt of strong alkali weak acid into water, preparing into a weakly alkaline solution, adding morpholine and 1-bromine-3-chloropropane into the weakly alkaline solution to carry out thermostatic reaction, standing and layering, and rectifying an oily matter at the upper layer to obtain intermediate N-(3-chloropropyl) morpholine; adding absolute ethyl alcohol and sodium hydroxide into a reaction kettle, then adding 4-butoxyphenol and N-(3-chloropropyl) morpholine, refluxing to obtain the oily matter, adding hydrochloric acid and methylbenzene into the oily matter, and layering to obtain an organic layer at the upper layer; adding a sodium hydroxide solution into a water layer at the lower layer to regulate the solution to be alkaline, then adding ethyl acetate and water and layering, and concentrating the solution at the upper layer to obtain a pramoxine basic group; and dissolving the pramoxine basic group into ethyl alcohol, and adding hydrochloric acid to obtain pramoxine dydrochloride. The preparation process disclosed by the invention requires no chlorination, production steps are reduced, the operation process is simple, the production cost is reduced, the environmental pollution problem is avoided, and large-scale industrial production can be realized.
Description
technical field [0001] The present invention relates to a kind of local anesthetic medicine, specifically a kind of preparation method of pramoxine hydrochloride. Background technique [0002] Pramocaine hydrochloride is a local anesthetic. Because pramoxine hydrochloride has a special chemical structure, it can reduce the risk of cross-allergic reactions. The production of pramoxine hydrochloride can produce surface anesthesia, and it is less irritating to the skin and non-delicate mucous membranes, and will not exceed the tolerable range. At present, the preparation method of pramoxine hydrochloride is: the product obtained by the reaction of morpholine and 3-chloropropanol is then chlorinated to prepare N-(3-chloropropyl)morpholine, N-(3-chloropropyl ) morpholine reacted with 4-butoxyphenol to prepare pramoxine hydrochloride. This reaction must have a chlorination step, the preparation step is longer, the production cost is higher, and the production efficiency is low....
Claims
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IPC IPC(8): C07D295/088
Inventor 于东海杨彦军胡俊峰王庭见
Owner 山东诚汇双达药业有限公司