Publication number: 20210171485
Abstract: The invention relates to the field of pharmaceutical synthesis, in particular to the preparation method of hexahydrofuro-furanol derivative, intermediates thereof and preparation methods thereof. The preparation methods comprises the steps of halogenation reaction, acylation reaction, enzymatic reduction reaction, reaction with amine compounds, reduction ring closure reaction (A1, A2, B, Cp1, CL, Cf) wherein, R1, R2, R3 are hydrogen or hydroxy protecting groups; R4 and R5 are the same or different and are phenyl, alkyl or substituted phenyl. In the preparation process of hexahydrofuro-furanol derivatives, the chirality is constructed by enzymatic method, and the product can be prepared with very high optical purity by adopting such technical means. The preparation method can be used to prepare the key intermediate, (3R, 3aS, 6aR)-hexahydrofuro[2,3-b]-3-ol, of Darunavir, in commercial production, which is a very economical route suitable for industrial production.
Type:
Application
Filed:
July 30, 2018
Publication date:
June 10, 2021
Applicant:
Jiangsu Ruike Medical Science And Technology Co., Ltd.
Inventors:
Zhaobo GAO, Jianhua CHEN, Zhidong WAN, Dawei HE, Zengle ZHOU, Xiaodong MA, Wei XIANG, Jingxin LIN, Yijiang MEI