1-(4-氯苯胺基)-4-(4-吡啶甲基)-2,3-二氮杂萘琥珀酸盐的合成与抑制肿瘤活性

摘要

l-(4-Chloroaniline)-4-(4-pyridylmethyl)-2, 3-benzodiazine succinate(4) was synthesized by addition, rearrangement, substitution and halogenesis steps with phthalide and 4-pyridinecarbaldehydes as starting reagents. The intermediate and target compound 4 were characterized by *H NMR, MS and HPLC. After purification by recrystallization, the compound 4 ( 98. 1 % purity estimated by HPLC ) was experimentally used to treat colorectal cancer nude mice. The result shows that this compound obviously restrains the growth of tumors.%研究了1-(4-氯苯胺基)4-(4-吡啶甲基)-2,3-二氮杂萘琥珀酸盐的合成工艺,采用苯酞和吡啶甲醛为起始原料,经加成、重排、取代和成盐4步反应得到目标化合物.中间体及目标化合物通过1H NMR、MS和HPLC进行了表征.重结晶纯化后的目标化合物纯度为98.1％.对荷瘤(人大肠癌HT 29细胞)裸鼠的抑癌活性测定表明,该化合物具有明显的抑制肿瘤生长作用.