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1. WO2020133411 - PREPARATION METHOD FOR EFINACONAZOLE

Publication Number WO/2020/133411
Publication Date 02.07.2020
International Application No. PCT/CN2018/125609
International Filing Date 29.12.2018
IPC
C07D 249/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
C07D 401/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
CPC
C07D 249/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
C07D 401/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • 威智医药有限公司 VIWIT PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 魏彦君 WEI, Yanjun
  • 王建 WANG, Jian
  • 邢艳平 XING, Yanping
Agents
  • 北京信诺创成知识产权代理有限公司 SINO-CREATIVITY INTELLECTUAL PROPERTY LAW FIRM
Priority Data
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PREPARATION METHOD FOR EFINACONAZOLE
(FR) PROCÉDÉ DE PRÉPARATION D'ÉFINACONAZOLE
(ZH) 一种艾氟康唑的制备方法
Abstract
(EN)
The present invention provides a preparation method for Efinaconazole, comprising the following steps: in the presence of bromide and base, subjecting (2R,3S)-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazole-1-yl)methyl]ethylene oxide and an inorganic acid salt of 4-methylenepiperidine to a cycloaddition reaction in a reaction solvent, to obtain Efinaconazole. The preparation method for Efinaconazole of the present invention has mild reaction conditions, high product yield, high purity, and low production costs, and is suitable for industrial production.
(FR)
La présente invention concerne un procédé de préparation d'éfinaconazole, comprenant les étapes suivantes : en présence de bromure et d'une base, soumettre du (2R,3S)-2-(2,4-difluorophényl))-3-méthyl-2-[(1H-1,2,4-triazol-1-yl) méthyl]éthylène et un sel d'acide inorganique de 4-méthylènepipéridine à une réaction de cycloaddition dans un solvant de réaction, pour obtenir de l'éfinaconazole. Le procédé de préparation de l'éfinaconazole de la présente invention présente des conditions de réaction douces, un rendement de produit élevé, une pureté élevée, et de faibles coûts de production, et est approprié pour une production industrielle.
(ZH)
本发明提供了一种艾氟康唑的制备方法,包括以下步骤:在溴化物和碱的存在下,在反应溶剂中,使(2R,3S)-2-(2,4-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]环氧乙烷与4-亚甲基哌啶的无机酸盐进行开环加成反应,以获得艾氟康唑。本发明的艾氟康唑的制备方法的反应条件温和,产品收率高、纯度高,生产成本低,适用于工业生产。
Also published as
KR1020217017538
EP2018944314
Latest bibliographic data on file with the International Bureau