| 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 |
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| 引用本文： | 蔡志强,孙铁民.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[J].合成化学,2009,17(6). |
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| 作者姓名： | 蔡志强 孙铁民 |
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| 作者单位： | 沈阳药科大学,制药工程学院,辽宁,沈阳,110016 |
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| 摘 要： | 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%.
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| 关 键 词： | 偶合反应 喹啉 药物合成 |
Synthesis of 6-Bromo-3-[2-(6-bromo-2-methoxyquinolin-3-yl)-1,2-diphenylethyl]-2-methoxyquinoline |
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| CAI Zhi-qiang,SUN Tie-min.Synthesis of 6-Bromo-3-[2-(6-bromo-2-methoxyquinolin-3-yl)-1,2-diphenylethyl]-2-methoxyquinoline[J].Chinese Journal of Synthetic Chemistry,2009,17(6). |
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| Authors: | CAI Zhi-qiang SUN Tie-min |
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| Abstract: | 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. |
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| Keywords: | TMC-207 TMC-207 coupling reaction quinoline drug synthesis |
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