2-氯-4-氟苯甲酸甲酯合成路线 (共 17 条)
反应条件
chloro-trimethyl-silane T=20°C; 24 h;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2004/46120 A2, 2004 ;
Location in patent: Page 175; 176 ;
WO 2004/046120 A2
反应条件
tetrabutyl ammonium fluoride in dimethyl sulfoxide T=25°C; 0.166667 h; Inert atmosphereMicrowave irradiationAnhydrous conditions;
参考文献
LaBeaume, Paul; Placzek, Michael; Daniels, Mathew; Kendrick, Ian; Ng, Patrick; McNeel, Melissa; Afroze, Roushan; Alexander, Abigail; Thomas, Rhiannon; Kallmerten, Amy E.; Jones, Graham B.
Tetrahedron Letters, 2010 , vol. 51, # 14 p. 1906 - 1909
反应条件
1: 61 percent / K2CO3 / 1-methyl-pyrrolidin-2-one / 5 h / 120 °C 2: 97 percent / 6 N aq. HCl; AcOH / 4 h / Heating View Scheme
参考文献
Kondo; Ogawa; Shinohara; Kurimura; Tanada; Kan; Yamashita; Nakamura; Hirano; Yamamura; Mori; Tominaga; Itai
Journal of Medicinal Chemistry, 2000 , vol. 43, # 23 p. 4388 - 4397
反应条件
conc. nitric acid in sulfuric acid
参考文献
Sumitomo Chemical Company, Limited
Patent: US4431822 A1, 1984 ;
反应条件
copper (I) cyanide in 1-methyl-pyrrolidin-2-one T=195°C; 1.5 h; Inert atmosphere;
参考文献
GILEAD CONNECTICUT, INC.; GENENTECH, INC.; CURRIE, Kevin S.; WANG, Xiaojing; YOUNG, Wendy B.
Patent: WO2012/31004 A1, 2012 ;
Location in patent: Page/Page column 113-114 ;
WO 2012/031004 A1
反应条件
in various solvent(s) T=195°C; 1.5 h;
参考文献
Wrobel, Jay; Dietrich, Arlene; Woolson, Shiela A.; Millen, Jane; McCaleb, Michael; et al.
Journal of Medicinal Chemistry, 1992 , vol. 35, # 24 p. 4613 - 4627
反应条件
potassium carbonate in 1-methyl-pyrrolidin-2-one T=120°C; 5 h;
参考文献
Kondo; Ogawa; Shinohara; Kurimura; Tanada; Kan; Yamashita; Nakamura; Hirano; Yamamura; Mori; Tominaga; Itai
Journal of Medicinal Chemistry, 2000 , vol. 43, # 23 p. 4388 - 4397
反应条件
1: 88 percent / K2CO3 / 1-methyl-pyrrolidin-2-one / 5 h / 120 °C 2: 60 percent / 5 N aq. NaOH / methanol / 15 h / Heating View Scheme
参考文献
Kondo; Ogawa; Shinohara; Kurimura; Tanada; Kan; Yamashita; Nakamura; Hirano; Yamamura; Mori; Tominaga; Itai
Journal of Medicinal Chemistry, 2000 , vol. 43, # 23 p. 4388 - 4397
反应条件
1-methyl-pyrrolidin-2-one; potassium carbonate T=120°C; 3 h;
参考文献
Tsukamoto, Issei; Koshio, Hiroyuki; Akamatsu, Seijiro; Kuramochi, Takahiro; Saitoh, Chikashi; Yatsu, Takeyuki; Yanai-Inamura, Hiroko; Kitada, Chika; Yamamoto, Eisaku; Sakamoto, Shuichi; Tsukamoto, Shin-ichi
Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 21 p. 9524 - 9535