马来酸氟吡汀的合成研究  

Synthesis of Flupidine Maleate

作　　者：吴为贲 吕磊 

机构地区：[1]江苏联环药业股份有限公司,江苏扬州225000

出　　处：《广州化工》2018年第4期22-24,共3页GuangZhou Chemical Industry

摘　　要：以6-硝基-2,5-二氨基吡啶和4-氟氯苄为起始原料经缩合得2-硝基-3-氨基-6-(4-氟苄胺基)吡啶,再经过氯化钙和硼氢化钠组合还原得到2,3-氨基-6-(4-氟苄胺基)吡啶,再与氯甲酸乙酯进行酰化反应,得到氟吡汀,再与马来酸成盐得到马来酸氟吡汀。此合成路线以6-硝基-2,5-二氨基吡啶和4-氟氯苄为原料,以氯化钙和硼氢化钠代替重金属催化氢化,具有较高安全性,较高收率,总收率为63.6%。6-nitro-2,5-pyridinediamine and α-Chloro-p-fluorotoluene were used as starting materials to obtain 2-nitro-3-amino-6-( 4-fluorobenzylamino) pyridine,and then reduced to give 2,3-amino-6-( 4-fluorobenzylamino)pyridine through combination of calcium chloride and sodium borohydride,followed by acylation with ethyl chloroformate to obtain flupirtine,and then salt with maleic acid to get flupirtine maleate. This route was based on 6-nitro-2,5-pyridinediamine and α-Chloro-p-fluorotoluene as raw materials,with calcium chloride and sodium borohydride instead of heavy metal catalytic hydrogenation,with higher safety and higher yield,the total yield was 63. 6%.

关 键 词：6-硝基-2 5-二氨基吡啶 4-氟氯苄 合成 

分 类 号：R914.5[医药卫生—药物化学]