含三氟甲基药物中间体的简便合成  

Facile Synthesis of Some Intermediates with Trifluoromethyl Group

作　　者：张靖[1] 陈拥军[2] 刘刚[1] 徐嵩[1] 

机构地区：[1]中国医学科学院北京协和医学院药物研究所,北京100050 [2]中国科学院化学所,北京100080

出　　处：《中国医药工业杂志》2011年第5期326-327,共2页Chinese Journal of Pharmaceuticals

摘　　要：用3,3,3-三氟丙酮酸甲酯为原料,在TiCl4作用下与对甲氧基苯酚等相应试剂经付-克反应,制得2-羟基-2-三氟甲基-2-(2-羟基-5-甲氧基苯基)乙酸甲酯(2a)、2-羟基-2-三氟甲基-2-(2,3-二羟基-5-甲基苯基)乙酸甲酯(2b)、2,7-二(1-羟基-1-甲氧羰基三氟乙基)-3-甲基吲哚(2c),收率分别为45%、73.2%和61.7%。With methyl 3,3,3-trifluoropyruvate as electrophilic agent in the presence of TiCl4 by Friedel-Crafts reaction,three intermediates,methyl 2-hydroxy-2-trifluoromethyl-2-(2-hydroxy-5-methoxyphenyl)acetate(2a),methyl 2-hydroxy-2-trifluoromethyl-2-(2,3-dihydroxy-5-methylphenyl)acetate(2b),and 2,7-bis(1-hydroxy-1-methoxycarbonyltrifluoroethyl)-3-methylindole(2c) were synthesized from the corresponding starting materials.The yields were 45%,73.2% and 61.7%,respectively.

关 键 词：3 3 3-三氟丙酮酸甲酯 尼罗替尼 比卡普胺 中间体 付-克反应 合成 

分 类 号：R9[医药卫生—药学]