116970-50-4Relevant articles and documents
Preparation method of compound fasudil hydrochloride
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Paragraph 0036; 0048-0049, (2021/09/11)
The invention relates to a novel efficient and economical method for synthesizing fasudil hydrochloride. The method comprises the following steps: carrying outsulfonamide and Boc protection on cheap and easily available ethylenediamine serving as a starting raw material in a synthesis route to obtain an intermediate tert-butyl-(N-(2-aminoethyl)-5-isoquinoline sulfonamide) carbamate (5), and carrying out collapse condensation to obtain fasudil hydrochloride. The method comprises four steps of nucleophilic substitution, deprotection, cyclization and salification. The total yield of the fasudil hydrochloride (1) is 67.1%, and the purity of the fasudil hydrochloride (1) is as high as 99.94%. Compared with a traditional process, high-price homopiperazine and derivatives thereof are prevented from being used as synthesis intermediates in the route, so the method has the advantages that raw materials are cheap and easy to obtain, operation is easy, cost is low, and the process is environmentally friendly and suitable for industrial production.