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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
凡德他尼
合成路线
（共 7 条）
50-00-0
甲醛
+
338992-12-4
N-(4-溴-2-氟苯基)-6-甲氧基-7-(哌啶-4-基甲氧基)喹唑啉-4-胺
→
反应条件
443913-73-3
凡德他尼
反应条件
NaBH(OAc)3; acetic acid in methanol; dichloromethane; water T=20°C; 2 h;
参考文献
Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226
50-00-0
甲醛
+
338992-20-4
4-((4-(4-溴-2-氟苯基氨基)-6-甲氧基喹唑啉-7-基氧基)甲基)哌啶-1-羧酸叔丁酯
→
反应条件
443913-73-3
凡德他尼
反应条件
1: With formic acid in water T=80°C; 6.5 - 8.5 h; 2: With potassium hydroxide in methanol; water T=60°C; 2 h; Product distribution / selectivity;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2007/36713 A2, 2007 ;
Location in patent: Page/Page column 59; 60 ;
WO 2007/036713 A2
367-24-8
4-溴-2-氟苯胺
+
264208-72-2
4-氯-6-甲氧基-7-[(1-甲基-4-哌啶基)甲氧基]-喹唑烷
→
反应条件
443913-73-3
凡德他尼
反应条件
in isopropyl alcohol T=80°C; 0.533333 h; Microwave irradiation;
参考文献
Marzaro, Giovanni; Guiotto, Adriano; Pastorini, Giovanni; Chilin, Adriana
Tetrahedron, 2010 , vol. 66, # 4 p. 962 - 968
367-24-8
4-溴-2-氟苯胺
→
反应条件
443913-73-3
凡德他尼
反应条件
1: hydrogenchloride / isopropyl alcohol / 2 h / Reflux 2: trifluoroacetic acid / 1 h / Reflux 3: potassium carbonate / N,N-dimethyl-formamide / 20 - 90 °C 4: trifluoroacetic acid / dichloromethane / 2 h / 20 °C 5: NaBH(OAc)3; acetic acid / methanol; dichloromethane; water / 2 h / 20 °C View Scheme
参考文献
Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226
162364-72-9
7-苄氧基-4-氯-6-甲氧基喹唑啉
→
反应条件
443913-73-3
凡德他尼
反应条件
1: hydrogenchloride / isopropyl alcohol / 2 h / Reflux 2: trifluoroacetic acid / 1 h / Reflux 3: potassium carbonate / N,N-dimethyl-formamide / 20 - 90 °C 4: trifluoroacetic acid / dichloromethane / 2 h / 20 °C 5: NaBH(OAc)3; acetic acid / methanol; dichloromethane; water / 2 h / 20 °C View Scheme
参考文献
Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226
196603-96-0
4-(4-溴-2-氟苯胺基)-7-羟基-6-甲氧基喹唑啉
→
反应条件
443913-73-3
凡德他尼
反应条件
1: potassium carbonate / N,N-dimethyl-formamide / 20 - 90 °C 2: trifluoroacetic acid / dichloromethane / 2 h / 20 °C 3: NaBH(OAc)3; acetic acid / methanol; dichloromethane; water / 2 h / 20 °C View Scheme
参考文献
Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226
768350-54-5
7-(苄氧基)-N-(4-溴-2-氟苯基)-6-甲氧基喹唑啉-4-胺
→
反应条件
443913-73-3
凡德他尼
反应条件
1: trifluoroacetic acid / 1 h / Reflux 2: potassium carbonate / N,N-dimethyl-formamide / 20 - 90 °C 3: trifluoroacetic acid / dichloromethane / 2 h / 20 °C 4: NaBH(OAc)3; acetic acid / methanol; dichloromethane; water / 2 h / 20 °C View Scheme
参考文献
Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy D.; Sledge, George W.; Zheng, Qi-Huang
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3222 - 3226
