Method for preparation of Efinaconazole

A compound and iodide technology, applied in the field of preparation of efluconazole, can solve the problems of consuming manpower and material resources, increasing operating procedures, and long reaction time, and achieve the effects of promoting technological progress, simplifying process operation, and easy handling
CN106565672AInactive Publication Date: 2017-04-19WATERSTONE PHARMA WUHAN
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
WATERSTONE PHARMA WUHAN
Publication Date
2017-04-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a method for preparation of Efinaconazole. The method comprises the following step: in the presence of iodide or its hydrate, in a reaction solvent and alkali, a compound as shown in the formula 2 is contacted with a compound as shown in the formula 3, so as to obtain a compound as shown in the formula 1. By the method, Efinaconazole can be effectively prepared. In addition, the method has advantages of few steps, simple synthesis process and mild reaction conditions. Meanwhile, excessive use of expensive amine can be avoided; yield and purity of the product are high; there are few by-products; production cost is low; corrosion to the reaction vessel during the production process is little; and industrial "three wastes (waste gas, waste water and industrial residue)" are easy to treat. The method is safe and environment-friendly, and is beneficial to industrial production of Efinaconazole.
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Description

technical field

[0001] The invention relates to the field of chemical synthesis, in particular, the invention relates to a method for preparing efluconazole. Background technique

[0002] The first topical triazole antifungal drug, Efinaconazole (compound represented by Formula 1), was developed for the treatment of local distal lateral subungual fungus (DLSO). DLSO is the most common onychomycosis. The pathogenic bacteria first invade the distal subungual nail bed, and the subungual horniness hyperplasia and thickening, the nail plate can become white, brown to taupe, the surface is uneven, tarnished, the nail plate missing, crunchy. Studies have found that efluconazole is effective against fungal diseases in both humans and animals.

[0003] The preparation of amino alcohols usually adopts the ring-opening addition reaction of amines to epoxides. Generally speaking, amines exist in the form of salts to facilitate storage, transportation and feeding. Usually the correspon...

Claims

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