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首先以异喹啉为原料,经氧化生成氮氧化物后与苯甲酰氯和水作用,得到1-羟基异喹啉,收率为73.3%.以Fasudil为原料,经氨基保护、氧化,在相转移催化剂的存在下,于二氯甲烷和水的两相体系中与苯甲酰氯和水作用,合成羟基Fasudil,HPLC纯度大于99%,总收率为46.8%,从而建立了一条条件温和、操作简便的羟基Fasudil的合成工艺路线.
First isoquinoline as raw material, the oxidation of nitrogen oxides with benzoyl chloride and water to give 1-hydroxyisoquinoline, the yield was 73.3%. Fasudil as raw material, the amino protection, oxidation, in the phase Transfer catalyzer with benzoyl chloride and water in a two-phase system of methylene chloride and water to synthesize hydroxyl Fasudil with a purity of more than 99% and a total yield of 46.8%, thus establishing a mild condition for operation Simple and convenient method of synthesis of hydroxyl Fasudil.