公开(公告)号：US20240287027A1

公开(公告)日：2024-08-29

申请号：US18570511

申请日：2022-05-26

Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY

Inventor： Jianhong ZHAO ,  Dingding WANG ,  Wulin YANG ,  Jinming NIU ,  Jun ZHU ,  Weiting WU ,  Jie YU ,  Zhen SUN ,  Xiaoli XU

IPC: C07D401/12

CPC classification number: C07D401/12

Abstract: An efficient and economical method for synthesizing Fasudil hydrochloride includes the synthesis route starts with inexpensive and readily available ethylenediamine as the starting material, obtains intermediate tert butyl-(N-(2-aminoethyl)-5-isoquinoline sulfonamide) carbamate (5) through sulfonylation and Boc protection, and then obtains Fasudil hydrochloride through a stacking process, which includes four steps: nucleophilic substitution, deprotection, cyclization, and salt formation. The total yield of Fasudil hydrochloride (1) is 67.1%, with a purity of up to 99.94%. Compared with traditional processes, the route avoids the use of expensive homopiperazine and its derivatives as synthetic intermediates. The advantages of the process include cheap and easy to obtain raw materials, simple operation, low cost, environmental friendliness, and suitability for industrial production.