Preparation method of mirabegron intermediate

Abstract

The invention provides a preparation method of a mirabegron intermediate. P-tert-butyloxycarborylaminobenzaldehyde is used as an initial raw material, six-step reaction is carried out to obtain a mirabegron intermediate with high yield; the method has the advantages of mild reaction conditions, convenience in operation, high purity of the obtained mirabegron intermediate, high yield and suitability for industrial production, so that a valuable synthetic route is provided for preparation of mirabegron, good social benefits and economic benefits can be brought, and the economic value potential is great.

Description

technical field [0001] The present invention relates to the technical field of organic compound synthesis pharmacy, more specifically, relate to the preparation method of a kind of Mirabegron intermediate that Mirabegron medicine is used in particular. Background technique [0002] Overactive bladder is a disease characterized by urgency, often accompanied by frequent urination and nocturia, which seriously affects the daily life and social life of patients. In recent years, with the arrival of my country's aging society and the increase of patients with diabetes and neurological diseases, the incidence of overactive bladder secondary to this has also increased year by year. Therefore seeking a kind of effective overactive bladder treatment drug is the key research direction of many institutions. [0003] Mirabegron is the first β3 adrenoceptor agonist drug for the treatment of overactive bladder. Mirabegron was developed by Astellas Pharmaceutical Company of Japan. A kind...

AI Technical Summary

Problems solved by technology

[0009] The disadvantages of this synthetic route are: long steps, cumbersome post-processing, time-consuming and labor-intensive, and low yield of the final product obtained, and the raw materials are expensive and costly, so it is not suitable for industrial production

[0012] The shortcoming of this synthesis route is: the borane used in the synthesis is highly toxic and dangerous, does not conform to the concept of green chemistry, and uses more reagents, and the cost is high, so it is not suitable for large-scale industrialization

[0015] The shortcoming of this synthetic route is: the potassium permanganate used in the synthesis has extremely high polluting property, can cause very big harm to the environment, and the starting material of reaction is difficult to obtain, and industrialized production is difficult

[0018] Prepare Mirabegron with this method, steps are few, and reaction is simple, but in the reaction process, by-product is more, and final product yield is not high, is not suitable for industrial large-scale production

[0019] In summary, the Mirabegron synthetic method of the prior art or steps are numerous and varied, or yield is low, or cost is high, thereby need a kind of simple and efficient synthetic method of Mirabegron

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