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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
101337-95-5
合成路线
（共 6 条）
367-21-5
3-氯-4-氟苯胺
+
333-20-0
硫氰化钾
+
96-32-2
溴乙酸甲酯
→
反应条件
101337-95-5
+
106016-81-3
反应条件
1: para-fluoro-meta-chloroaniline; potassium thioacyanate With bromine in acetic acid T=15 - 20°C; 1.5 h; 2: With ammonium hydroxide in water pH=11 - 12; 3: bromoacetic acid methyl ester
参考文献
GLAXO GROUP LIMITED; BERTANI, Barbara; CREMONESI, Susanna; GARZYA, Vincenzo; MICHELI, Fabrizio; RUPCIC, Renata; SABBATINI, Fabio Maria
Patent: WO2011/151361 A1, 2011 ;
Location in patent: Page/Page column 49-50 ;
WO 2011/151361 A1
917474-04-5
+
79-11-8
氯乙酸
→
反应条件
101337-95-5
反应条件
1: 2-amino-6-chloro-5-fluorobenzenethiol With sodium hydroxide 0.5 h; Reflux; 2: chloroacetic acid in water 1.5 h; Reflux;
参考文献
Armenise, Domenico; Muraglia, Marilena; Florio, Marco Antonio; De Laurentis, Nicolino; Rosato, Antonio; Carrieri, Antonio; Corbo, Filomena; Franchini, Carlo
Archiv der Pharmazie, 2012 , vol. 345, # 5 p. 407 - 416
367-21-5
3-氯-4-氟苯胺
+
333-20-0
硫氰化钾
+
79-11-8
氯乙酸
→
反应条件
101337-95-5
+
106016-81-3
反应条件
sodium hydroxide; bromine Yield given. Multistep reaction. Yields of byproduct given;
参考文献
Cecchetti, Violetta; Fravolini, Arnaldo; Fringuelli, Renata; Mascellani, Giuseppe; Pagella, Piergiuseppe; et al.
Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 465 - 473
101337-93-3
7-氯-6-氟-1,3-苯并噻唑-2-胺
→
反应条件
101337-95-5
反应条件
1.1: sodium hydroxide / 24 h / Reflux 2.1: sodium hydroxide / 0.5 h / Reflux 2.2: 1.5 h / Reflux View Scheme
参考文献
Armenise, Domenico; Muraglia, Marilena; Florio, Marco Antonio; De Laurentis, Nicolino; Rosato, Antonio; Carrieri, Antonio; Corbo, Filomena; Franchini, Carlo
Archiv der Pharmazie, 2012 , vol. 345, # 5 p. 407 - 416
101337-95-5
→
反应条件
101337-87-5
N-去甲基芦氟沙星
反应条件
1: 90 percent / LiAlH4 / tetrahydrofuran / 1 h / Ambient temperature 2: 2.) polyphosphoric acid / 1.) 120 deg C, 2 h, 2.) 160 deg C, 1 h 3: 78.7 percent / 15 percent NaOH / 0.75 h / Heating 4: 53.8 percent / KBr, Pb(OAc)4 / H2O; acetic acid / 30 °C 5: toluene / 3 h / Heating 6: 89 percent / PCl3 / dimethylformamide / 2 h / Ambient temperature View Scheme
参考文献
Cecchetti, Violetta; Fravolini, Arnaldo; Fringuelli, Renata; Mascellani, Giuseppe; Pagella, Piergiuseppe; et al.
Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 465 - 473
101337-95-5
→
反应条件
101363-10-4
芦氟沙星
反应条件
1: 90 percent / LiAlH4 / tetrahydrofuran / 1 h / Ambient temperature 2: 2.) polyphosphoric acid / 1.) 120 deg C, 2 h, 2.) 160 deg C, 1 h 3: 78.7 percent / 15 percent NaOH / 0.75 h / Heating 4: 53.8 percent / KBr, Pb(OAc)4 / H2O; acetic acid / 30 °C 5: toluene / 3 h / Heating 6: 59 percent / PCl3 / dimethylformamide / 2 h / Ambient temperature View Scheme
参考文献
Cecchetti, Violetta; Fravolini, Arnaldo; Fringuelli, Renata; Mascellani, Giuseppe; Pagella, Piergiuseppe; et al.
Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 465 - 473
