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Technique for synthesizing levorotatory betaxolol hydrochloride

A technology for the synthesis of betaxolol hydrochloride, which is applied in the field of synthesis of L-betaxolol hydrochloride, can solve the problems of high operational skill requirements, long production cycle, and high price, and achieve simple process methods and three-waste emissions Small, easy-to-operate effect

Inactive Publication Date: 2007-12-12
ZHENGZHOU UNIV
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Problems solved by technology

[0009] Unfortunately, in the above-mentioned synthesis process, except that most steps need nitrogen protection, the reagents and catalysts used in the synthesis process such as diethylzinc and diiodomethane are relatively expensive, and diethylzinc is in the air. Medium energy spontaneous combustion. Contact with moist air, chlorine, and oxidants may cause combustion hazards. Therefore, this step of the reaction requires the reaction system to be absolutely anhydrous, requires very high operating skills in the production process, and is highly toxic; Long, so that the whole production cycle is relatively long, about 50 days; and the first step yield is relatively low, resulting in a very low total yield of the process, which is 16.7%. In addition, the reagents and catalysts used are expensive, making the cost very high. Disadvantages make this process difficult for industrial production

Method used

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  • Technique for synthesizing levorotatory betaxolol hydrochloride

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Embodiment Construction

[0030] For a better description of the present invention, examples are as follows:

[0031] The preparation of embodiment L-betaxolol hydrochloride (compound 6)

[0032] (1) Preparation of Compound 2 (2-(4-benzyloxy)phenylethanol)

[0033] Dissolve p-hydroxyphenethyl alcohol (27.60g, 0.2mol) and benzyl chloride (50.40g, 0.4mol) in an organic solvent, then add sodium hydroxide (16.00g, 0.4mol) and stir mechanically, heat at 70°C for 10 Hour. After the reaction, the solid was removed by filtration, the filtrate was concentrated and evaporated to dryness, and water was added for recrystallization to obtain 44.23 g of 2-(4-benzyloxy)phenylethanol, with a yield of 97%. The experimental data are as follows:

[0034] C 15 h 16 o 2 , 1 HNMR (400MHz, CDCl 3 ): δ7.44-7.25(m, 5H), 7.14(d, 2H, J=8.5Hz), 6.93(d, 2H, J=8.5Hz), 5.05(s, 2H), 3.82(t, 2H, J=6.6Hz), 2.81(t, 2H, J=6.5Hz); 13 CNMR (100.6MHz, CDCl 3 ): δ157.51, 137.06, 130.67, 129.99, 128.58, 127.94, 127.45, 114.98, 70.02...

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Abstract

The invention discloses a method for synthesizing left-handed hydrochloric betaxolol. It employs tyrosol as raw material, and comprises benzyl protection, alkanisation, pulling off protection, alkanisation, aminating and getting high- enantiotropy product. The invention is characterized by simple operation, easy get raw material, low toxicity, safe and convenient operation, low pollution, high productivity and short period.

Description

technical field [0001] The present invention relates to the synthesis of organic compounds, in particular to the synthesis process of L-betaxolol hydrochloride. Background technique [0002] L-betaxolol hydrochloride was launched in the United States in February 2000 under the trade name "Betaxon". The drug is mainly used to reduce intraocular pressure in patients with chronic open-angle glaucoma or ocular hypertension. Glaucoma, the gradual damage to the optic nerve due to increased pressure inside the eye, is a very serious eye disease. This type of disease can lead to vision loss, rapid onset, great harm, and blindness at any time. It is a common and difficult eye disease. In recent years, the incidence rate has increased. According to the statistics of the World Health Organization, there are currently about 67 million glaucoma patients worldwide, and about 4.5 million people have lost vision due to glaucoma. In my country, the incidence of primary glaucoma The rate is...

Claims

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Application Information

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IPC IPC(8): C07C217/34C07C213/02
Inventor 刘宏民张京玉
Owner ZHENGZHOU UNIV
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