Preparation method for ethambutol hydrochloride

Abstract

The invention discloses a preparation method for ethambutol hydrochloride. The preparation method comprises the following steps: 1) mixing S-(+)-2-amino-1-butanol with the specific rotation of +8.3 degrees to +9.3 degrees and 1,2-dichloroethane in a reactor and reacting to obtain a reaction discharged material; 2) transferring the reaction discharged material into a separation system; after addingalkali, separating out the S-(+)-2-amino-1-butanol and returning the separated S-(+)-2-amino-1-butanol back to the reactor; 3) adding alcohol into a separation system again to obtain an alcohol solution containing ethambutol; 4) separating the obtained alcohol solution of the ethambutol to remove salt, so as to obtain a desalted alcohol solution containing the ethambutol; 5) cooling the desaltedalcohol solution containing the ethambutol and separating to remove impurities, so as to obtain an impurity-removed alcohol solution of the ethambutol; 6) adding the alcohol solution of the ethambutolinto water to regulate the water content of a system; then adding the alcohol and hydrogen chloride to obtain an alcohol solution containing the ethambutol hydrochloride; and 7) separating the ethambutol hydrochloride through crystallization, so as to obtain the ethambutol hydrochloride.

Description

technical field [0001] The application belongs to the technical chemistry field of medicine preparation, and more specifically, the application relates to a preparation method of ethambutol hydrochloride. Background technique [0002] Ethambutol hydrochloride is widely used in combination with other anti-tuberculosis drugs to treat tuberculosis caused by Mycobacterium tuberculosis, and can also be used in the treatment of tuberculous meningitis and atypical mycobacterial infection. The drug accounts for more than 13% of the anti-TB drug market share. [0003] Ethambutol hydrochloride (English name is Ethambutol Hydrochloride), its chemical name is [2R,2[S-(R * , R * )-R](+)-2,2,-(1,2-Ethylenediimino)-bis-1-butanol dihydrochloride, the molecular formula is C 10 h 24 N 2 o 2 HCl, the molecular weight is 277.23, the CAS number is 1070-11-7, and its structural formula is: [0004] [0005] The currently reported synthesis methods include 1,2-epoxy-3-butene, (S)-2-amino...

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Problems solved by technology

[0006] And take 1,2-epoxy-3-butene as the method for starting raw material to prepare ethambutol hydrochloride has following shortcoming: because 1,2-epoxy-3-butene is gas, increased equipment complexity, It is difficult to control the amount of feed, and there are too many synthesis processes

[0007] With (S)-2-aminobutyric acid ethyl ester as the shortcoming of the method for starting raw material: raw material is difficult to obtain, and price is more expensive, and production cost is too high

[0008] However, the method of protecting the amino group first and then condensing also has the following disadvantages: too many types of raw materials, relatively complicated operations, many impurities in the product, and difficult to scale application

Therefore, this method takes a long time for the equipment and consumes a lot of energy, which limits the production progress of large-scale production rolling feeding

Moreover, HCl gas is not easy to transport. If it is self-made, it will produce a large amount of strong acid waste liquid, which is difficult to handle.

Therefore, this method limits the application of large-scale production

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