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Preparation method and application of 1-[(4-hydroxyethyl) phenoxy]-3-(isopropylamino) propan-2-ol

A technology of isopropylamino and phenoxy, which is applied in the field of detection of related substances in betaxolol hydrochloride and betaxolol hydrochloride eye drops, can solve the problems of preparation, synthesis and application that have not been reported in domestic literature, Affect the quality and safety of betaxolol hydrochloride products, and achieve the effect of simple and controllable preparation process, good economic and social benefits, and easy operation

Pending Publication Date: 2020-09-22
SHANDONG INST FOR FOOD & DRUG CONTROL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Betaxolol impurity A is a white solid powder that is easily soluble in water and is a degradation product produced during the storage of betaxolol hydrochloride, which is a potential hidden danger that affects the quality and safety of betaxolol hydrochloride products
In the field of research on related substances of betaxolol hydrochloride, the preparation and detection methods of betaxolol impurity A are proposed for the first time, and its preparation, synthesis method and application have not been reported in domestic literature

Method used

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  • Preparation method and application of 1-[(4-hydroxyethyl) phenoxy]-3-(isopropylamino) propan-2-ol
  • Preparation method and application of 1-[(4-hydroxyethyl) phenoxy]-3-(isopropylamino) propan-2-ol
  • Preparation method and application of 1-[(4-hydroxyethyl) phenoxy]-3-(isopropylamino) propan-2-ol

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1) The synthesis reaction equation of compound A is as follows:

[0030]

[0031] The reactants and products used in the reaction are shown in Table 1.

[0032] Table 1

[0033]

[0034] The specific reaction steps are shown in Table 2.

[0035] Table 2

[0036]

[0037] (2) The final product reaction equation is as follows:

[0038]

[0039] The reactants and products used in the reaction are shown in Table 3.

[0040] table 3

[0041]

[0042] The specific reaction steps are shown in Table 4.

[0043] Table 4

[0044]

[0045] The synthesized compound was identified by H NMR spectrum and mass spectrometry, and the spectra were as follows: figure 1 and figure 2 As shown, the identification structure is correct.

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Abstract

The invention belongs to the technical field of medicine preparation, and mainly relates to a preparation method of a compound 1-[(4-hydroxyethyl) phenoxy]-3-(isopropylamino) propyl-2-ol and application of the compound in betalol hydrochloride and betalol hydrochloride eye drops related substance detection. The synthetic route of the preparation method is shown in the specification. The 1-[(4-hydroxyethyl) phenoxy]-3-(isopropylamino) propan-2-ol prepared by the preparation method can be used as a reference substance; the method is used for detecting the content of 1-[(4-hydroxyethyl) phenoxy]-3-(isopropylamino) propan-2-ol in betalol hydrochloride and eye drops of betalol hydrochloride and analyzing and identifying components of betalol hydrochloride. Technical support and material guarantee are provided for improving the quality standard of betalol hydrochloride and eye drops thereof and controlling the safety of product quality so that the national standard of betalol hydrochloride is at the world leading level, and the betalol hydrochloride eye drops have good economic benefits and social benefits.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and mainly relates to the preparation method of compound 1-[(4-hydroxyethyl)phenoxy]-3-(isopropylamino)propan-2-ol and the preparation method of betaxolol hydrochloride and Application of betaxolol hydrochloride eye drops in the detection of related substances. Background technique [0002] Betaxolol hydrochloride is a selective B1 receptor blocker, which hardly blocks B2 receptors, has calcium ion antagonism, has no endogenous sympathomimetic activity, has a certain membrane stabilizing effect, and can inhibit aqueous humor Produce and increase the outflow of aqueous humor to reduce intraocular pressure, which can reduce the increase in intraocular pressure caused by glaucoma or other eye diseases. Clinically based on this mechanism, it is mainly used to treat open-angle glaucoma, angle-closure glaucoma that is not fully controlled after surgery, and ocular hypertension. The main ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C213/04C07C217/32G01N30/86G01N30/06G01N30/02
CPCC07C213/04C07D303/26C07D301/28G01N30/02G01N30/06G01N30/8675C07C217/32
Inventor 徐玉文李玉梅郑静郭常川
Owner SHANDONG INST FOR FOOD & DRUG CONTROL