2-氟-4-甲酰基苯甲酸甲酯合成路线 （共 7 条）
反应条件
hydrogen; acetic acid; nickel in water
T=20°C; 18 h;
参考文献
Giranda, Vincent L.; Penning, Thomas D.; Gandhi, Virajkamar B.; Thomas, Sheela A.; Zhu, Gui-Dong; Gong, Jianchun
Patent: US2007/259937 A1, 2007 ;
Location in patent: Page/Page column 13 ;
反应条件
1: 2-Fluoro-4-formyl Benzoic Acid With sodium hydride in N,N-dimethyl-formamide
T=0 - 20°C;
2: methyl iodide in N,N-dimethyl-formamide
2 h;
参考文献
INCYTE CORPORATION; RODGERS, James, D.; LI, Yun-Long; SHEPARD, Stacey; WANG, Haisheng
Patent: WO2011/28685 A1, 2011 ;
Location in patent: Page/Page column 75 ;
WO 2011/028685 A1
反应条件
1.1: N-bromosuccinmide / dibenzoyl peroxide / tetrachloromethane / 40 h / Reflux
2.1: silver nitrate / ethanol; water / 0.75 h / 50 °C
2.2: 20 °C
3.1: sodium hydride / N,N-dimethyl-formamide / 0 - 20 °C
3.2: 2 h
View Scheme
参考文献
INCYTE CORPORATION; RODGERS, James, D.; LI, Yun-Long; SHEPARD, Stacey; WANG, Haisheng
Patent: WO2011/28685 A1, 2011 ;
WO 2011/028685 A1
反应条件
1: With N-bromosuccinmide; dibenzoyl peroxide in tetrachloromethane
2: With water; silver nitrate in tert-butyl alcohol
Further stages.;
参考文献
Sakaki, Junichi; Kishida, Masashi; Konishi, Kazuhide; Gunji, Hiroki; Toyao, Atsushi; Matsumoto, Yuki; Kanazawa, Takanori; Uchiyama, Hidefumi; Fukaya, Hiroaki; Mitani, Hironobu; Arai, Yoshie; Kimura, Masaaki
Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 17 p. 4804 - 4807
反应条件
bis-triphenylphosphine-palladium(II) chloride; carbon monoxide in N,N-dimethyl-formamide
T=110°C; 2 h;
参考文献
Zimmerman, Sommer S.; Khatri, Alpa; Garnier-Amblard, Ethel C.; Mullasseril, Praseeda; Kurtkaya, Natalie L.; Gyoneva, Stefka; Hansen, Kasper B.; Traynelis, Stephen F.; Liotta, Dennis C.
Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2334 - 2356
反应条件
1.1: silver nitrate / ethanol; water / 0.75 h / 50 °C
1.2: 20 °C
2.1: sodium hydride / N,N-dimethyl-formamide / 0 - 20 °C
2.2: 2 h
View Scheme
参考文献
INCYTE CORPORATION; RODGERS, James, D.; LI, Yun-Long; SHEPARD, Stacey; WANG, Haisheng
Patent: WO2011/28685 A1, 2011 ;
WO 2011/028685 A1
反应条件
1: methanol; tetrahydrofuran / 1 h / 0 - 20 °C
2: bis-triphenylphosphine-palladium(II) chloride; carbon monoxide / N,N-dimethyl-formamide / 2 h / 110 °C
View Scheme
参考文献
Zimmerman, Sommer S.; Khatri, Alpa; Garnier-Amblard, Ethel C.; Mullasseril, Praseeda; Kurtkaya, Natalie L.; Gyoneva, Stefka; Hansen, Kasper B.; Traynelis, Stephen F.; Liotta, Dennis C.
Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2334 - 2356
