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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
21384-43-0
合成路线
（共 23 条）
21384-43-0
→
反应条件
303162-38-1
反应条件
1.1: BuLi / tetrahydrofuran; hexane / 0.5 h / 0 °C 1.2: 81 percent / tetrahydrofuran; hexane / -78 - 20 °C 2.1: 86 percent / Br2; AcOH / 3 h / 80 °C 3.1: 63 percent / dimethylformamide / 14 h / 20 °C 4.1: 95 percent / NaOH / ethanol; H2O / 2 h / 20 °C 5.1: 72 percent / 0.25 h / 140 °C View Scheme
参考文献
Miwatashi, Seiji; Arikawa, Yasuyoshi; Kotani, Etsuo; Miyamoto, Maki; Naruo, Ken-Ichi; Kimura, Hiroyuki; Tanaka, Toshimasa; Asahi, Satoru; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5966 - 5979
21384-43-0
→
反应条件
303162-93-8
反应条件
1.1: BuLi / tetrahydrofuran; hexane / 0.5 h / 0 °C 1.2: 81 percent / tetrahydrofuran; hexane / -78 - 20 °C 2.1: 86 percent / Br2; AcOH / 3 h / 80 °C 3.1: 71 percent / dimethylformamide / 14 h / 20 °C 4.1: Et3N / tetrahydrofuran / 3 h / 20 °C 5.1: HCl / tetrahydrofuran; H2O / 14 h / 40 °C View Scheme
参考文献
Miwatashi, Seiji; Arikawa, Yasuyoshi; Kotani, Etsuo; Miyamoto, Maki; Naruo, Ken-Ichi; Kimura, Hiroyuki; Tanaka, Toshimasa; Asahi, Satoru; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5966 - 5979
21384-43-0
→
反应条件
303162-78-9
反应条件
1.1: BuLi / tetrahydrofuran; hexane / 0.5 h / 0 °C 1.2: 81 percent / tetrahydrofuran; hexane / -78 - 20 °C 2.1: 86 percent / Br2; AcOH / 3 h / 80 °C 3.1: 71 percent / dimethylformamide / 14 h / 20 °C 4.1: 77 percent / Et3N / tetrahydrofuran / 1 h / 20 °C View Scheme
参考文献
Miwatashi, Seiji; Arikawa, Yasuyoshi; Kotani, Etsuo; Miyamoto, Maki; Naruo, Ken-Ichi; Kimura, Hiroyuki; Tanaka, Toshimasa; Asahi, Satoru; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5966 - 5979
461-87-0
2-氟-4-甲基吡啶
+
21384-43-0
→
反应条件
303162-49-4
反应条件
1: 2-fluoro-4-methyl-pyridine With lithium diisopropyl amide in tetrahydrofuran; hexane T=-10°C; 1 h; 2: 1-(3-methylbenzoyl)-2-methylaziridine in tetrahydrofuran; hexane T=-78°C; 2 h;
参考文献
Miwatashi, Seiji; Arikawa, Yasuyoshi; Kotani, Etsuo; Miyamoto, Maki; Naruo, Ken-Ichi; Kimura, Hiroyuki; Tanaka, Toshimasa; Asahi, Satoru; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5966 - 5979
461-87-0
2-氟-4-甲基吡啶
→
反应条件
303162-49-4
反应条件
diisopropylamine in tetrahydrofuran; water
参考文献
Ohkawa, Shigenori; Naruo, Ken-ichi; Miwatashi, Seiji; Kimura, Hiroyuki
Patent: US2004/53973 A1, 2004 ;
US 20040053973 A1
21384-43-0
→
反应条件
303162-79-0
N-(4-(2-乙基-4-(3-甲基苯基)噻唑-5-基)吡啶-2-基)苯甲酰胺
反应条件
1.1: BuLi / tetrahydrofuran; hexane / 0.5 h / 0 °C 1.2: 81 percent / tetrahydrofuran; hexane / -78 - 20 °C 2.1: 86 percent / Br2; AcOH / 3 h / 80 °C 3.1: 60 percent / dimethylformamide / 14 h / 20 °C 4.1: Et3N / tetrahydrofuran / 3 h / 20 °C 5.1: 59.8 g / HCl / tetrahydrofuran; H2O / 14 h / 40 °C View Scheme
参考文献
Miwatashi, Seiji; Arikawa, Yasuyoshi; Kotani, Etsuo; Miyamoto, Maki; Naruo, Ken-Ichi; Kimura, Hiroyuki; Tanaka, Toshimasa; Asahi, Satoru; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5966 - 5979
→
反应条件
325770-44-3
反应条件
diisopropylamine in tetrahydrofuran; water
参考文献
Ohkawa, Shigenori; Naruo, Ken-ichi; Miwatashi, Seiji; Kimura, Hiroyuki
Patent: US2004/53973 A1, 2004 ;
US 20040053973 A1
21384-43-0
+
108-47-4
2,4-二甲基吡啶
→
反应条件
325770-44-3
反应条件
1: 2,4-dimethyl-pyridine With lithium diisopropyl amide in tetrahydrofuran; hexane T=-10°C; 1 h; 2: 1-(3-methylbenzoyl)-2-methylaziridine in tetrahydrofuran; hexane T=-78°C; 2 h;
参考文献
Miwatashi, Seiji; Arikawa, Yasuyoshi; Kotani, Etsuo; Miyamoto, Maki; Naruo, Ken-Ichi; Kimura, Hiroyuki; Tanaka, Toshimasa; Asahi, Satoru; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5966 - 5979
21384-43-0
→
反应条件
325769-02-6
反应条件
1.1: LDA / tetrahydrofuran; hexane / 1 h / -10 °C 1.2: 65 percent / tetrahydrofuran; hexane / 2 h / -78 °C 2.1: Br2; AcOH / 3 h / 80 °C 3.1: 84 percent / dimethylformamide / 14 h / 20 °C View Scheme
参考文献
Miwatashi, Seiji; Arikawa, Yasuyoshi; Naruo, Ken-Ichi; Igaki, Keiko; Watanabe, Yasumasa; Kimura, Hiroyuki; Kawamoto, Tomohiro; Ohkawa, Shigenori
Chemical and Pharmaceutical Bulletin, 2005 , vol. 53, # 4 p. 410 - 418
21384-43-0
→
反应条件
365428-80-4
反应条件
1.1: BuLi / tetrahydrofuran; hexane / 0.5 h / 0 °C 1.2: 81 percent / tetrahydrofuran; hexane / -78 - 20 °C 2.1: 86 percent / Br2; AcOH / 3 h / 80 °C 3.1: 63 percent / dimethylformamide / 14 h / 20 °C View Scheme
参考文献
Miwatashi, Seiji; Arikawa, Yasuyoshi; Kotani, Etsuo; Miyamoto, Maki; Naruo, Ken-Ichi; Kimura, Hiroyuki; Tanaka, Toshimasa; Asahi, Satoru; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5966 - 5979
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