CAJ | 학술논문

改进抗癌新药瑞戈非尼的合成工艺，以2-吡啶甲酸为原料通过卤化，酰胺化，得到4-氯-N-甲基吡啶-2-甲酰胺，成盐酸盐得到4-氯-N-甲基吡啶-2-甲酰胺盐酸盐，与3-氟-4-氨基苯酚亲核取代反应得到4-（4-氨基-3-氟苯氧基）-N-甲基吡啶-2-甲酰胺，然后和4-氯-3-三氟甲基苯异氰酸酯缩合反应得到瑞戈非尼，总收率为47%。
개진항암신약서과비니적합성공예，이2-필정갑산위원료통과서화，선알화，득도4-록-N-갑기필정-2-갑선알，성염산염득도4-록-N-갑기필정-2-갑선알염산염，여3-불-4-안기분분친핵취대반응득도4-（4-안기-3-불분양기）-N-갑기필정-2-갑선알，연후화4-록-3-삼불갑기분이청산지축합반응득도서과비니，총수솔위47%。
This study is to synthesize the new anticancer drug regorafenib and improve the process. The 4-chloro-N-methylpyridine-2-carboxamide hydrochloride was synthesized from pyridine-2-carboxylic acid by chlorination, amidation and then it was reacted with 3-fluoro-4-aminophenol, through nucleophileic substitution to give 4-(4-amino-3-fluorophenoxy)-N-methylpyridine-2-carboxamide, and then it was con-densed with 4-chloro-3-(trifluoromethyl) phenyl isocyanate to form regorafenib with an overall yield of 47%.