Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Technique of synthesizing levorotatory betaxolol hydrochloride

A technology of betaxolol hydrochloride and synthesis process, which is applied in the field of synthesis technology of L-betaxolol hydrochloride, can solve the problems of expensive reagents and catalysts, high requirements on operation skills, low total process yield and the like, and achieves production scale Small, high optical purity, high chemical purity effect

Inactive Publication Date: 2007-08-08
刘宏民
View PDF4 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Technique of synthesizing levorotatory betaxolol hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0030] The preparation of embodiment L-betaxolol hydrochloride (compound 6)

[0031] (1) Preparation of Compound 1 (S-1-(4-(2-hydroxyethyl)phenoxy)-2,3-propylene oxide)

[0032] Dissolve p-hydroxyphenylethyl alcohol (27.60g, 0.2mol) and R-epichlorohydrin (18.50g, 0.4mol) in an organic solvent, then add sodium hydroxide (16.00g, 0.4mol) and stir mechanically, at 60°C Heated for 8 hours. After the reaction was completed, the sodium carbonate was removed by filtration, the filtrate was concentrated and evaporated to dryness, and ethyl acetate was added for recrystallization to obtain 36.10 g of S-1-(4-(2-hydroxyethyl)phenoxy)-2,3-propylene oxide , yield 93%, experimental data are as follows:

[0033] C 11 h 14 o 3 , Mp 39°C, [α] D 20 =+12.0°(c1.00, CH 3 OH); υ _ = 3349,2945,2929,2873,1613 , 1513,1245,1047,1027,906,848,823 c m - ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07C213/02C07C217/34
Inventor 刘宏民张京玉张正
Owner 刘宏民
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products