1-羟基异喹啉及羟基Fasudil的合成  

Synthesis of 1-Isoquinolinol and Hydroxyfasudil

作　　者：陈美珠[1] 刘帅[1] 王欣然[1] 罗浩[1] 陈立功[1] 王东华[2] 

机构地区：[1]天津大学化工学院精细化工系,天津300072 [2]天津大学药物科学与技术学院,天津300072

出　　处：《有机化学》2012年第2期404-408,共5页Chinese Journal of Organic Chemistry

摘　　要：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.1-Isoquinolinol was synthesized from isoquinoline via oxidation,reaction with benzoyl chloride and water in yield of 73.3%.According to this process,a method for the synthesis of hydroxyfasudil [1-（1-hydroxy-5-isoquinolinesulfonyl）-ho-mopiperazine] from fasudil [hexahydro-1-（5-isoquinoline-sulfonyl）-1H-1,4-diazepine] was estabilshed in this paper.The proc-ess undergoes effectively through protection for amino,oxidation,reaction with water in a water/dichloromethane biphase system in the presence of phase transfer catalyst and benzoyl chloride and then deprotection.The objective product was finally obtained in yield of 46.8% with a purity more than 99%（HPLC）.It is virtually a practical process with mild reaction condi-tions and simple operation.

关 键 词：1-羟基异喹啉 氮氧化物 FASUDIL 羟基Fasudil 

分 类 号：TQ463.53[化学工程—制药化工]