A kind of synthetic method of gamithromycin

A technology of gamimycin and its synthesis method, which is applied in chemical instruments and methods, organic chemistry, bulk chemical production, etc. It can solve the problems of high difficulty in purification, high toxicity of waste liquid, and medium purity of gamimycin, etc., and achieves The reaction conditions are easy to control, realize industrialized large-scale production, and improve the effect of purity and yield
CN112300221BActive Publication Date: 2022-04-15AMICOGEN CHINA BIOPHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
AMICOGEN CHINA BIOPHARM CO LTD
Publication Date
2022-04-15

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Abstract

The invention discloses a method for synthesizing gamithromycin, which uses 9-deoxy-8a-aza-8a-homoerythromycin A as a raw material, and diaces with propionaldehyde in a protic solvent under the catalysis of an organic acid. Alcohol reaction forms propyral 9-deoxy-8a-aza-8a-homoerythromycin A, then reduces through boron reducing agent, removes protecting group under acidic conditions, obtains gamithromycin; preparation process of the present invention The yield of the obtained gamithromycin product can reach more than 92.0% before post-treatment, after recrystallization treatment, its purity can reach more than 99.0%, the overall yield can reach more than 90.0%, and the reaction process is mild, Able to realize industrialized mass production.
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Description

technical field

[0001] The invention relates to the technical field of chemical synthesis, in particular to a synthesis method of gamithromycin. Background technique

[0002] Gamithromycin is a semi-synthetic 15-membered azamacrolide antibacterial drug, which is usually used for the prevention and treatment of cattle disease caused by pathogenic bacteria such as Mannella hemolyticus, Pasteurella multocida, and Histophilia somnolus. Respiratory system diseases; Gamithromycin is used for food animals. It has the advantages of broad antibacterial spectrum, strong antibacterial activity, single administration, long half-life, fast absorption, high bioavailability, and low residue, which is in line with the development trend of veterinary drugs in my country. Good clinical application value and broad market prospect.

[0003] At present, the synthesis of gamithromycin generally takes deoxyazaerythromycin as the reaction substrate, and adopts different methods to introduce propyl g...

Claims

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