摘要
本研究合成了抗非酒精性脂肪肝(NAFLD)药物Selonsertib(1)。3-氟-4-溴-6-氨基甲苯(18),在以N,N-二甲基甲酰胺作溶剂,N2氛围下与溴甲基环丙基酮(3)缩合得到2-((5-溴-4-氟-2-甲基苯基)氨基)-1-环丙基乙基-1-酮(4),制备(4)的反应时间缩短,反应条件温和,收率55.4%。制备化合物5-(4-环丙基-1H-咪唑-1-基)-2-氟-4-甲基苯甲酸(7)时,用环己基氯化镁代替异丙基氯化镁,同时后处理改用异丙醚重结晶,在保证(7)的收率的同时,对环境更加友好,也使析晶操作更易进行。
In this study,Selonsertib(1),an non-alcoholic fatty liver disease drug,was synthesized.5-bromo-4-fluoro-2- methylaniline (18) condensed with2-bromo-1- cyclopropylethanone in anhydrous N,N- dimethylformamide under nitrogen to give2-[(5- bromo-4-fluoro-2-methylphenyl)amino]-1- cyclopropylethanone (4).The time for the preparation of (4) is shortened,the reaction conditions are mild,and the yield is 55.4%. Cyclohexanemagnesium chloride was used to prepare the compound (7),and the crude was pured by recrystallization in isopropyl ether,which ensures the yield of compound (7),is more environmentally friendly and makes crystallization easier.
作者
胡孔泉
郑琳日
陈国华
Hu Kongquan;Zheng Linri;Chen Guohua(College of Pharmacy,China Pharmaceutical University,Nanjing 210000,China)
出处
《山东化工》
CAS
2019年第17期48-50,53,共4页
Shandong Chemical Industry
