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1. WO2020108146 - PREPARATION METHOD FOR LEPIMECTIN, AND INTERMEDIATE THEREOF

Publication Number WO/2020/108146
Publication Date 04.06.2020
International Application No. PCT/CN2019/111554
International Filing Date 17.10.2019
IPC
C07D 493/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
22in which the condensed system contains four or more hetero rings
CPC
C07D 493/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
22in which the condensed system contains four or more hetero rings
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of products other than chlorine, adipic acid, caprolactam, or chlorodifluoromethane, e.g. bulk or fine chemicals or pharmaceuticals
55Synthetic design, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • 浙江海正药业股份有限公司 ZHEJIANG HISUN PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 张绍勇 ZHANG, Shaoyong
  • 王继栋 WANG, Jidong
  • 张辉 ZHANG, Hui
  • 李建宋 LI, Jiansong
  • 齐欢 QI, Huan
  • 滕云 TENG, Yun
  • 白骅 BAI, Hua
Priority Data
201811416685.226.11.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PREPARATION METHOD FOR LEPIMECTIN, AND INTERMEDIATE THEREOF
(FR) PROCÉDÉ DE PRÉPARATION DE LEPIMECTINE ET SON INTERMÉDIAIRE
(ZH) 一种乐平霉素的制备方法及其中间体
Abstract
(EN)
Disclosed are a preparation method for lepimectin as shown in a formula V and an intermediate thereof. Tenvermectin is used as initial raw material. The method comprises: acid hydrolysis with a 5-hydroxyl protecting group, reaction with 2-methoxy-imino phenylacetic acid through SN2, and finally removing the 5-hydroxyl protecting group to obtain a compound of formula V. Advantages: low cost, high purity, high yield and suitability for industrial production.
(FR)
L’invention concerne un procédé de préparation de lepimectine et son intermédiaire. Tenvermectine est utilisé comme matière première initiale. Le procédé comprend : l’hydrolyse acide avec un groupe protecteur 5-hydroxyle, la mise en réaction avec un acide phénylacétique 2-méthoxy-imino via SN2 et l’élimination finale du groupe protecteur 5-hydroxyle en vue de l’obtention d’un composé de formule V. Avantages : faible coût, pureté élevée, haut rendement et se prêtant à la production industrielle.
(ZH)
本发明公开了一种式V所示的乐平霉素的制备方法及其中间体,以天维菌素为起始原料,分别经过酸水解反应,5位羟基上保护基,然后与2-甲氧亚氨基苯乙酸经过SN2反应,最后脱除5位羟基保护基得到式V化合物。本发明具有成本低,纯度高,收率高和适合工业化生产的优点。
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