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Preparation method for 2-(2-methoxyphenoxy)ethylamine

A technology of methoxyphenoxy and ethylamine, applied in the field of preparation of 2-ethylamine, can solve problems such as high production cost and low yield, and achieve the effect of reducing production cost

Inactive Publication Date: 2019-01-15
TONGREN UNIV
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Problems solved by technology

In the prior art, there is a blocking reaction in the reaction of guaiacol and 1,2-dichloroethane, so that the yield of 2-(2-methoxyphenoxy)chloroethane is lower than 60%, and the final 2 The total yield of -(2-methoxyphenoxy)ethylamine is only 43%, resulting in high production cost of 2-(2-methoxyphenoxy)

Method used

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  • Preparation method for 2-(2-methoxyphenoxy)ethylamine
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  • Preparation method for 2-(2-methoxyphenoxy)ethylamine

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Embodiment Construction

[0013] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some, not all, embodiments of the present invention. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0014] see figure 1 :

[0015] In the route of the reaction of guaiacol and 2-dichloroethane in the route [I], because the halogen elements at both ends of 2-dichloroethane do not have a high degree of selectivity, by-products are easily generated, resulting in low yield and a large amount of pollution. , and NaN3 has a certain toxicity and is easy to explode when it meets water, so it is not suitable for chemical production

[0016] The ammoniation of halog...

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Abstract

The invention provides a preparation method for 2-(2-methoxyphenoxy)ethylamine. The preparation method comprises the following steps: synthesizing 2-(2-methoxyphenoxy)ethanol with guaiacol as a starting material; then synthesizing 2-(2-methoxyphenoxy)chloroethane through chlorination; then reacting 2-(2-methoxyphenoxy)chloroethane with potassium phthalimide to obtain N-(o-methoxyphenoxyethyl)-phthalimide; and finally, performing basic hydrolysis to obtain 2-(2-methoxyphenoxy)ethylamine. The yields of the above four steps of reactions are that the yield of 2-(2-methoxyphenoxy)ethanol is 98.9%;the yield of 2-(2-methoxyphenoxy)chloroethane is 93.7%; the yield of N-(o-methoxyphenoxyethyl)-phthalimide is 86.4%; the yield of 2-(2-methoxyphenoxy)ethylamine is 91.2%; and the total yield of the four steps is 73.04%, which is higher than the yield of 43% in conventional production processes. The preparation method of the invention reduces the production cost of 2-(2-methoxyphenoxy)ethylamine and is safe in the production process.

Description

technical field [0001] The invention relates to the technical field of preparation of carvedilol raw materials, in particular to a preparation method of 2-(2-methoxyphenoxy)ethylamine. Background technique [0002] 2-(2-methoxyphenoxy)ethylamine is an important intermediate in the synthesis of the β-receptor blocker carvedilol, which is a drug for the treatment of essential hypertension. Used alone or in combination with other antihypertensive drugs, especially thiazide diuretics, carvedilol can also be used to treat symptomatic congestive heart failure, which can reduce mortality and hospitalization rates for cardiovascular events, and improve patient general conditions and slow down disease progression. In the prior art, there is a blocking reaction in the reaction of guaiacol and 1,2-dichloroethane, so that the yield of 2-(2-methoxyphenoxy)chloroethane is lower than 60%, and the final 2 The total yield of -(2-methoxyphenoxy)ethylamine is only 43%, which causes 2-(2-meth...

Claims

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Application Information

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IPC IPC(8): C07C213/02C07C217/20
CPCC07C41/22C07C41/26C07C68/065C07C213/02C07D209/48C07C69/96C07C43/23C07C43/225C07C217/20
Inventor 张玲钰王霜霜王涛李秀美李修刚
Owner TONGREN UNIV
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