US 12,258,330 B2
Method for preparing voriconazole and intermediate thereof
Wenxiang Zhou, Xunqiao (CN); Wenfeng Huang, Xunqiao (CN); and Jiaxing Hu, Xunqiao (CN)
Assigned to Zhejiang Huahai Pharmaceutical Co., Ltd., Xunqiao (CN); and Zhejiang Huahai LiCheng Pharmaceutical Co., Ltd., Xunqiao (CN)
Appl. No. 17/430,794
Filed by Zhejiang Huahai Pharmaceutical Co., Ltd., Xunqiao (CN); and Zhejiang Huahai LiCheng Pharmaceutical Co., Ltd., Xunqiao (CN)
PCT Filed Feb. 18, 2020, PCT No. PCT/CN2020/075707
§ 371(c)(1), (2) Date Aug. 13, 2021,
PCT Pub. No. WO2020/169025, PCT Pub. Date Aug. 27, 2020.
Claims priority of application No. 201910121961.0 (CN), filed on Feb. 19, 2019.
Prior Publication US 2022/0162189 A1, May 26, 2022
Int. Cl. C07D 403/06 (2006.01)
CPC C07D 403/06 (2013.01) 15 Claims
 
1. A method for preparing voriconazole intermediate, comprising the following steps: reacting a compound 2 or a salt thereof as a starting material under an acidic condition and subjecting to a post-treatment to obtain a compound 3 and a compound 4:

OG Complex Work Unit Chemistry
wherein the compound 2 is a substance with a configuration of 2S,3S or 2R,3R or 2S,3R or 2R,3S in two chiral centers, or a mixture of two or more of the above substances.