4-氨基-5-氯-2-甲氧基苯甲酸合成路线 （共 38 条）
反应条件
1: 4-Amino-5-chloro-2-methoxy benzoic acid With 4-methyl-morpholine; 2-chloro-4,6-dimethoxy-[1,3,5]triazine in N,N-dimethyl-formamide T=20°C; 1 h; 2: N-[2-(ethylamino)ethyl]amine in N,N-dimethyl-formamide T=20°C; 19 h;
参考文献
NEKTAR THERAPEUTICS; CHENG, Lin; RIGGS-SAUTHIER, Jennifer; ANAND, Neel, K.
Patent: WO2014/43707 A1, 2014 ;
Location in patent: Paragraph 0166; 0167 ;
反应条件
silver carbonate; copper dichloride; palladium dichloride in tetrahydrofuran T=110°C; 24 h;
参考文献
Peng, Xuefeng; Shao, Xiang-Feng; Liu, Zhong-Quan
Tetrahedron Letters, 2013 , vol. 54, # 24 p. 3079 - 3081
反应条件
1: 4-Amino-5-chloro-2-methoxy benzoic acid With chloroformic acid ethyl ester; triethylamine in tetrahydrofuran 2: C15H23FN2O2 in tetrahydrofuran T=20°C; 16 h;
参考文献
Davies, Stephen G.; Huckvale, Rosemary; Lorkin, Thomas J.A.; Roberts, Paul M.; Thomson, James E.
Tetrahedron Asymmetry, 2011 , vol. 22, # 14-15 p. 1591 - 1593
反应条件
1: triethylamine / tetrahydrofuran / 2 h / 0 °C 2: tetrahydrofuran / 16 h / 0 - 20 °C View Scheme
参考文献
Davies, Stephen G.; Huckvale, Rosemary; Lee, James A.; Lorkin, Thomas J.A.; Roberts, Paul M.; Thomson, James E.
Tetrahedron, 2012 , vol. 68, # 15 p. 3263 - 3275
反应条件
dimethylsulfide borane complex in chlorobenzene T=80 - 130°C; 21 h;
参考文献
Bedford, Robin B.; Betham, Michael
Journal of Organic Chemistry, 2006 , vol. 71, # 25 p. 9403 - 9410
反应条件
1: thionyl chloride / 5 h / 80 °C 2: acetic acid / 5 h / 50 °C 3: nitric acid / 0.42 h / 20 °C View Scheme
参考文献
US2012/277224 A1, ;
US 20120277224 A1
反应条件
1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride in dichloromethane 4 h; Ambient temperature; Yield given;
参考文献
Journal of Medicinal Chemistry, , vol. 34, # 2 p. 616 - 624
反应条件
hydrogenchloride; triethylamine in chloroform
参考文献
Hokuriku Pharmaceutical Co.,Ltd
Patent: EP306827 B1, 1991 ;
反应条件
1: Et3N / CHCl3 / 0.5 h / Ambient temperature 2: CHCl3 / 14 h / Ambient temperature View Scheme
参考文献
Sakaguchi; Nishino; Ogawa; Iwanaga; Yasuda; Kato; Ito
Chemical and Pharmaceutical Bulletin, 1992 , vol. 40, # 1 p. 202 - 211
反应条件
chloroformic acid ethyl ester; triethylamine 1.) CHCl3, -10 deg C, 1 h, 2.)a) from -10 deg C to -5 deg C, 1 h, b) RT; Yield given. Multistep reaction;
参考文献
Kato; Morie; Hino; Kon; Naruto; Yoshida; Karasawa; Matsumoto
Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1406 - 1413
