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1. WO2013149577 - NEW SYNTHESIS PROCESS OF ANTIPARASITIC DRUG SELAMECTIN

Publication Number WO/2013/149577
Publication Date 10.10.2013
International Application No. PCT/CN2013/073604
International Filing Date 02.04.2013
IPC
C07H 17/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
17Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
04Heterocyclic radicals containing only oxygen as ring hetero atoms
08Hetero rings containing eight or more ring members, e.g. erythromycins
CPC
C07H 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
C07H 17/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
17Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
04Heterocyclic radicals containing only oxygen as ring hetero atoms
08Hetero rings containing eight or more ring members, e.g. erythromycins
Applicants
  • 浙江海正药业股份有限公司 ZHEJIANG HISUN PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 尹明星 YIN, Mingxing
  • 吴健超 WU, Jianchao
  • 柴健 CHAI, Jian
Agents
  • 北京集佳知识产权代理有限公司 UNITALEN ATTORNEYS AT LAW
Priority Data
201210102405.703.04.2012CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) NEW SYNTHESIS PROCESS OF ANTIPARASITIC DRUG SELAMECTIN
(FR) NOUVEAU PROCÉDÉ DE SYNTHÈSE DU MÉDICAMENT ANTIPARASITAIRE SÉLAMECTINE
(ZH) 抗寄生虫药赛拉菌素的合成新工艺
Abstract
(EN) Provided in the present invention are novel key intermediates of Selamectin and the preparation method thereof. Also provided is a new synthesis process, using Doramectin as a starting material, and obtaining Selamectin via hydrogenation, oxidation, oximation and desugaring. The new process of the present invention has few steps, and is simple to operate, high in yield, low in cost and causes little pollution, and is more suitable for large scale industrial production.
(FR) La présente invention concerne de nouveaux intermédiaires clefs de sélamectine et leur procédé de préparation. Un nouveau procédé de synthèse, utilisant de la doramectine comme matériau de départ, et donnant de la sélamectine via hydrogénation, oxydation, oximation et élimination de sucre, est également décrit. Le nouveau procédé de la présente invention présente peu d'étapes et est simple à exploiter, de rendement élevé, peu coûteux et provoque peu de pollution, et convient mieux pour une production industrielle à grande échelle.
(ZH) 本发明提供了新颖的赛拉菌素关键中间体及其制备方法;本发明还提供了一种赛拉菌素的合成新工艺,该工艺以朵拉克汀为起始原料,通过氢化反应,氧化反应,肟化、脱糖得到赛拉菌素。本发明的新工艺步骤少,操作简单,收率高,成本低,污染小,更加适合大规模的工业化生产。
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