文档介绍：有机化学Chinese Journal anic ChemistryNOTE * E-mail: ******@tju. Received May 25,2011; revised August 29, 2011; accepted October 21, 2011. 404 http://sioc-/ ? 2012 Chinese Chemical Society & SIOC, CASChin. J. Org. Chem. 2012, 32, 404~408DOI: -羟基异喹啉及羟基Fasudil的合成陈美珠a刘帅a王欣然a罗浩a陈立功a王东华*,b(a天津大学化工学院精细化工系天津 300072)(b天津大学药物科学与技术学院天津 300072) 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, %. 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%, %, 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. 关键词 1-羟基异喹啉; 氮氧化物; Fasudil; 羟基Fasudil Synthesis of 1-Isoquinolinol and Hydroxyfasudil Chen, Meizhua Liu, Shuaia Wang, Xinrana Luo, HaoaChen, Ligonga Wang, Donghua*,b(aInstitute of Chemical Engineering and Technology, Tianjin University, Tianjin 300072)(b School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072)Abstract 1-Isoquinolinol was synthesized from isoquinoline via oxidation, reaction with benzoyl chloride and water in yieldof %. 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/dichloromet