313996-78-0Relevant articles and documents
Preparation method of genotoxic fasudil hydrochloride impurities
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Paragraph 0028, (2020/06/05)
The invention relates to a preparation method of genotoxic fasudil hydrochloride impurities. The preparation method specifically comprises the following steps: preparing the fasudil hydrochloride impurities including methyl 5-isoquinolinesulfonate, ethyl 5-isoquinolinesulfonate, methyl 8-isoquinolinesulfonate, ethyl 8-isoquinolinesulfonate, methyl 5-quinolinesulfonate, ethyl 5-quinolinesulfonate,methyl 8-quinolinesulfonate and ethyl 8-quinolinesulfonate: firstly preparing isoquinolinesulfonyl chloride hydrochloride or quinolinesulfonyl chloride hydrochloride from isoquinoline sulfonic acid orquinoline sulfonic acid used as an initial raw material and thionyl chloride, and then reacting the isoquinolinesulfonyl chloride hydrochloride or quinolinesulfonyl chloride hydrochloride with methylalcohol and ethyl alcohol respectively to generate the corresponding fasudil hydrochloride methyl ester and ethyl ester impurities. The invention also provides a method for synthesizing the genotoxicfasudil hydrochloride impurityies with high purity to solve the problems of poor stability, easy rearrangement and easy decomposition of methyl quinolinesulfonate and ethyl ester.