Technique of synthesizing levorotatory betaxolol hydrochloride

Abstract

The invention discloses a synthesizing technique of left-handed hydrochloric betamicin, which comprises the following steps: adopting p-hydroxyphenethylol and R-epoxy halogen propane as original raw material; alkylating; aminating; protecting; alkylating; removing protection; obtaining pure high-antimer left-handed betamicin and hydrochlorate.

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...

AI Technical Summary

Problems solved by technology

[0009] Unfortunately, in the above 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 and contact with humid air, chlorine, and oxidants may cause combustion hazards, so this step of the reaction requires the reaction system to be absolutely anhydrous, requiring very high operating skills in the production process and high toxicity; in addition, the reaction time of the second step of the reaction is too long , so that the entire production cycle is relatively long; the low yield of the first step leads to a very low total yield of the process, and the reagents and catalysts used are expensive, making the cost very high. The above disadvantages make this process difficult to industrialize production

Images