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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
奥卡西平
合成路线
（共 56 条）
39507-06-7
→
反应条件
28721-07-5
奥卡西平
反应条件
1.1: pyridine / toluene / 24 h / 50 °C 1.2: pyridine / 22 h / 100 °C 2.1: 90 percent / aq. NaOH / methanol / 24 h / 25 °C 3.1: polyphosphoric acid / 3 h / 95 °C 4.1: 97 percent / aq. NaOH / 6 h / 100 °C 5.1: 98 percent / dimethylformamide / 4 h / 24 °C 6.1: 98 percent / Et3N; DMAP / CH2Cl2 / 3.5 h / 20 - 40 °C 7.1: 95 percent / hydrogen / Pd/C / methanol / 3 h / 30 °C 8.1: 40 percent / polyphosphoric acid / toluene / 11 h / 110 °C 9.1: aq. Na2CO3 / methanol; H2O / 0.5 h / 23 °C 10.1: CH2Cl2 / 17 h / 25 °C 10.2: 70 percent / H2O View Scheme
参考文献
Kaufmann, Daniel; Fuenfschilling, Peter C.; Beutler, Ulrich; Hoehn, Pascale; Lohse, Olivier; Zaugg, Werner
Tetrahedron Letters, 2004 , vol. 45, # 27 p. 5275 - 5278
805236-74-2
→
反应条件
28721-07-5
奥卡西平
反应条件
1.1: 90 percent / aq. NaOH / methanol / 24 h / 25 °C 2.1: polyphosphoric acid / 3 h / 95 °C 3.1: 97 percent / aq. NaOH / 6 h / 100 °C 4.1: 98 percent / dimethylformamide / 4 h / 24 °C 5.1: 98 percent / Et3N; DMAP / CH2Cl2 / 3.5 h / 20 - 40 °C 6.1: 95 percent / hydrogen / Pd/C / methanol / 3 h / 30 °C 7.1: 40 percent / polyphosphoric acid / toluene / 11 h / 110 °C 8.1: aq. Na2CO3 / methanol; H2O / 0.5 h / 23 °C 9.1: CH2Cl2 / 17 h / 25 °C 9.2: 70 percent / H2O View Scheme
参考文献
Kaufmann, Daniel; Fuenfschilling, Peter C.; Beutler, Ulrich; Hoehn, Pascale; Lohse, Olivier; Zaugg, Werner
Tetrahedron Letters, 2004 , vol. 45, # 27 p. 5275 - 5278
353497-35-5
→
反应条件
28721-07-5
奥卡西平
反应条件
1.1: polyphosphoric acid / 3 h / 95 °C 2.1: 97 percent / aq. NaOH / 6 h / 100 °C 3.1: 98 percent / dimethylformamide / 4 h / 24 °C 4.1: 98 percent / Et3N; DMAP / CH2Cl2 / 3.5 h / 20 - 40 °C 5.1: 95 percent / hydrogen / Pd/C / methanol / 3 h / 30 °C 6.1: 40 percent / polyphosphoric acid / toluene / 11 h / 110 °C 7.1: aq. Na2CO3 / methanol; H2O / 0.5 h / 23 °C 8.1: CH2Cl2 / 17 h / 25 °C 8.2: 70 percent / H2O View Scheme
参考文献
Kaufmann, Daniel; Fuenfschilling, Peter C.; Beutler, Ulrich; Hoehn, Pascale; Lohse, Olivier; Zaugg, Werner
Tetrahedron Letters, 2004 , vol. 45, # 27 p. 5275 - 5278
95-53-4
邻甲苯胺
→
反应条件
28721-07-5
奥卡西平
反应条件
1: 91 percent / NaOtBu / Pd(OAc)2; rac-BINAP / toluene 2: 82 percent / NaH / dimethylformamide 3: 70 percent / LDA; TMEDA; n-BuLi / tetrahydrofuran; hexane / 1 h / -20 °C 4: 70 percent / Rh(PPh3)3Cl 5: 80 percent View Scheme
参考文献
Lohse, Olivier; Beutler, Ulrich; Fuenfschilling, Peter; Furet, Pascal; France, Julien; Kaufmann, Daniel; Penn, Gerhard; Zaugg, Werner
Tetrahedron Letters, 2001 , vol. 42, # 3 p. 385 - 389
76041-86-6
N,N-二乙基-2-溴苯甲酰胺
→
反应条件
28721-07-5
奥卡西平
反应条件
1: 88 percent / NaOtBu / Pd(OAc)2; rac-BINAP / toluene 2: 97 percent / NaH / dimethylformamide 3: 86 percent / LDA; TMEDA; n-BuLi / tetrahydrofuran; hexane / 4 h / -20 °C 4: 75 percent / TMSCl; NaI / acetonitrile 5: 80 percent View Scheme
参考文献
Lohse, Olivier; Beutler, Ulrich; Fuenfschilling, Peter; Furet, Pascal; France, Julien; Kaufmann, Daniel; Penn, Gerhard; Zaugg, Werner
Tetrahedron Letters, 2001 , vol. 42, # 3 p. 385 - 389
1027035-99-9
→
反应条件
28721-07-5
奥卡西平
反应条件
1: 97 percent / NaH / dimethylformamide 2: 86 percent / LDA; TMEDA; n-BuLi / tetrahydrofuran; hexane / 4 h / -20 °C 3: 75 percent / TMSCl; NaI / acetonitrile 4: 80 percent View Scheme
参考文献
Lohse, Olivier; Beutler, Ulrich; Fuenfschilling, Peter; Furet, Pascal; France, Julien; Kaufmann, Daniel; Penn, Gerhard; Zaugg, Werner
Tetrahedron Letters, 2001 , vol. 42, # 3 p. 385 - 389
54616-47-6
2-溴-N,N-二甲基苯甲酰胺
→
反应条件
28721-07-5
奥卡西平
反应条件
1: 91 percent / NaOtBu / Pd(OAc)2; rac-BINAP / toluene 2: 82 percent / NaH / dimethylformamide 3: 70 percent / LDA; TMEDA; n-BuLi / tetrahydrofuran; hexane / 1 h / -20 °C 4: 70 percent / Rh(PPh3)3Cl 5: 80 percent View Scheme
参考文献
Lohse, Olivier; Beutler, Ulrich; Fuenfschilling, Peter; Furet, Pascal; France, Julien; Kaufmann, Daniel; Penn, Gerhard; Zaugg, Werner
Tetrahedron Letters, 2001 , vol. 42, # 3 p. 385 - 389
353497-28-6
→
反应条件
28721-07-5
奥卡西平
反应条件
1: 82 percent / NaH / dimethylformamide 2: 70 percent / LDA; TMEDA; n-BuLi / tetrahydrofuran; hexane / 1 h / -20 °C 3: 70 percent / Rh(PPh3)3Cl 4: 80 percent View Scheme
参考文献
Lohse, Olivier; Beutler, Ulrich; Fuenfschilling, Peter; Furet, Pascal; France, Julien; Kaufmann, Daniel; Penn, Gerhard; Zaugg, Werner
Tetrahedron Letters, 2001 , vol. 42, # 3 p. 385 - 389
332081-66-0
→
反应条件
28721-07-5
奥卡西平
反应条件
1: 70 percent / LDA; TMEDA; n-BuLi / tetrahydrofuran; hexane / 1 h / -20 °C 2: 70 percent / Rh(PPh3)3Cl 3: 80 percent View Scheme
参考文献
Lohse, Olivier; Beutler, Ulrich; Fuenfschilling, Peter; Furet, Pascal; France, Julien; Kaufmann, Daniel; Penn, Gerhard; Zaugg, Werner
Tetrahedron Letters, 2001 , vol. 42, # 3 p. 385 - 389
332081-67-1
→
反应条件
28721-07-5
奥卡西平
反应条件
1: 72 percent / LDA; TMEDA; n-BuLi / tetrahydrofuran; hexane / 2 h / -20 °C 2: 70 percent / Rh(PPh3)3Cl 3: 80 percent View Scheme
参考文献
Lohse, Olivier; Beutler, Ulrich; Fuenfschilling, Peter; Furet, Pascal; France, Julien; Kaufmann, Daniel; Penn, Gerhard; Zaugg, Werner
Tetrahedron Letters, 2001 , vol. 42, # 3 p. 385 - 389
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