Title:
METHOD FOR SYNTHESIZING SELAMECTIN
Document Type and Number:
WIPO Patent Application WO/2023/082574
Kind Code:
A1
Abstract:
The present invention provides a method for synthesizing selamectin, specifically comprising: oxidizing doramectin by means of manganese dioxide, oximating and desugaring same by using a hydroxylamine hydrochloride aqueous solution in a one-step method, and finally selectively reducing same under the effect of a Wilkinson catalyst and hydrogen to obtain selamectin. In the present invention, C-5 hydroxyl of a raw material doramectin is oxidized into carbonyl, and the generation of impurities in a follow-up reaction process is reduced. Tert-butyl alcohol having a large steric hindrance is used as a solvent, thus preventing transesterification impurities that are generated when methyl alcohol or isopropyl alcohol is used as a solvent; and a hydrogenation reaction is carried out in the last step, and a crude product is purified and then put into the hydrogenation reaction, thus reducing catalyst consumption, and greatly reducing costs. The method of the present invention has a relatively high yield, and the total yield reaches 57%. HPLC quality analysis is carried out on a pure selamectin product, the purity being 97.11%, and known impurities and unknown impurities meeting pharmacopeia requirements. The present invention provides a simpler, more economical and more efficient synthesis method, and is suitable for industrial production.
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Inventors:
CHEN RENER (CN)
ZHONG XIUWEN (CN)
HUANG YOUCHUN (CN)
ZHANG LEI (CN)
CHEN WENTENG (CN)
YU YONGPING (CN)
ZHONG XIUWEN (CN)
HUANG YOUCHUN (CN)
ZHANG LEI (CN)
CHEN WENTENG (CN)
YU YONGPING (CN)
Application Number:
PCT/CN2022/092181
Publication Date:
May 19, 2023
Filing Date:
May 11, 2022
Export Citation:
Assignee:
ZHEJIANG RONGYAO BIOTECH CO LTD (CN)
UNIV ZHEJIANG (CN)
UNIV ZHEJIANG (CN)
International Classes:
C07H1/00; C07H17/08
Domestic Patent References:
| WO2017055502A1 | 2017-04-06 |
Foreign References:
| CN114106071A | 2022-03-01 | |||
| CN1099394A | 1995-03-01 | |||
| CN1266437A | 2000-09-13 | |||
| CN103360444A | 2013-10-23 |
Attorney, Agent or Firm:
HANGZHOU QIUSHI PATENT OFFICE CO., LTD. (CN)
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