6-溴-3-2-(6-溴-2-甲氧基喹啉-3-基)-1,2-二苯乙基-2-甲氧基喹啉的合成

摘要

A new type of anti-TB drug of quinoline-TMC-207 derivative, 6-bromo-3-[2-(6-bromo-2-methoxyquinolin-3-yl)-1,2-diphenylethyl]-2-methoxyquinoline, was synthesized from 6-bromo-3-(chlorophenylmethyl)-2-methoxyquinoline(2) by coupling reaction and the structure was confirmed by ~1H NMR and HR-MS. The optimum reaction conditions at 80 ℃ for 6 h were as follows: 2 was 10 mmol; Et_3N was 5 mL; KI was 0.17 g; MeCN was 150 mL. The yield was 73% under the conditions.%以6-溴-3-(氯苯基甲基)-2-甲氧基喹啉(2)为起始原料,经过偶合对接反应合成了新型喹啉类抗结核药物TMC-207的衍生物6-溴-3-[2-(6-溴-2-甲氧基喹啉-3-基)-1,2-二苯乙基]-2-甲氧基喹啉,其结构经1H NMR和HR-MS确证.最佳反应条件:2 10 mmol,Et_3N 5 mL,KI 0.17 g,乙腈150 mL,于80 ℃反应6 h,收率73%.