The present invention provides efinaconazole producing and purifying methods adapted to industrial scale that provide high-purity efinaconazole in high yield by simple operations using specific impurities as indices. The efinaconazole producing method comprises:
step A of forming a toluene solution comprising compound (II), compound (III), an inorganic base, and toluene in a volume (L) which is 2 to 5 times the mass (kg) of compound (II);
step B of subjecting the toluene solution to reaction under heating;
step C of washing the reaction mixture from step B to obtain a toluene solution of crude efinaconazole in which the residual amount of 4-MP is not more than 5 wt % of efinaconazole.
本发明提供了适应工业规模的依
芬康唑生产和提纯方法,该方法以特定杂质为指标,通过简单的操作即可高产提供高纯度的依
芬康唑。生产依
芬康唑的方法包括
步骤 A 形成
甲苯溶液,该
甲苯溶液由化合物 (II)、化合物 (III)、
无机碱和
甲苯组成,体积 (L) 是化合物 (II) 质量 (kg) 的 2 至 5 倍;
步骤 B 将
甲苯溶液加热反应
步骤 C:洗涤步骤 B 中的反应混合物,以获得粗制依
芬康唑的
甲苯溶液,其中 4-MP 的残留量不超过依
芬康唑重量的 5%。