Daebong Ls Co., Ltd.

Eun Ju Park

Jin Oh Park

Hyun Ji

Ji Eun Lee

Eun Mi Kim

The present invention relates to a co-crystalline form of efinaconazole and a pharmaceutically acceptable coformer forming a co-crystalline phase. The present invention also relates to a method for preparing the co-crystalline form. The co-crystallization product of efinaconazole according to the present invention meets all requirements for use as an active ingredient of a pharmaceutical composition and is highly stable to heat and other one or more other ingredients of the composition. Therefore, the co-crystallization product of efinaconazole is suitable for use in the preparation of pharmaceuticals. In addition, the method of the present invention enables the preparation of the co-crystallization product of efinaconazole in a simple and easy manner on a commercial scale.

Co-crystalline form of efinaconazole and method for preparing the same

A solid dispersion of amorphous efinaconazole and a method for preparing the same are proposed. The solid dispersion includes an amorphous form of efinaconazole and at least one stabilization carrier selected from hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), ethyl cellulose (EC), hydroxypropyl methylcellulose acetate succinate (HPMC-AS), polyvinylpyrrolidone (PVP), polyacrylic acid (PAA), saccharin, and malonic acid. The solid dispersion undergoes minimal thermodynamic deformation when exposed to ambient temperature and humidity, achieving improved stability, while maintaining the inherent improved stability and bioavailability of amorphous efinaconazole.

Amorphous efinaconazole solid dispersion

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.

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Hwaseong-si, South Korea

Eun Ju Park