Method for preparing efinaconazole using ionic liquid as medium
US12018010B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 25, 2020 |
| Grant date | Jun 25, 2024 |
| Priority date | — |
| Expiry date | Jun 27, 2041 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D249/08
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention relates to a novel method for preparing efinaconazole using an ionic liquid as a medium. The method includes subjecting 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole to a coupling reaction with 4-methylenepiperidine or an organic chemically acceptable salt thereof in the presence of a base and an ionic liquid compound. The base makes the 4-methylenepiperidine or organic chemically acceptable salt thereof anionic. The use of the ionic liquid in the method of the present invention prevents the formation of related substances, shortens the reaction time, and enables easy preparation of the final compound efinaconazole in high purity and yield on a large scale, compared to the use of organic solvents in conventional methods.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.