4-氨基-5-氯-2-甲氧基苯甲酸合成路线 （共 38 条）
反应条件
1: 81 percent / BH3*SMe2 / chlorobenzene / 21 h / 80 - 130 °C
2: 81.5 percent / NaOtBu; Pd(OAc)2; [HP-t-Bu3][BF4] / toluene / 3 h / 160 °C / microwave irradiation
3: 61.5 percent / NaOtBu; Pd(OAc)2; [HP-t-Bu3][BF4] / dioxane / 18 h / Heating
View Scheme
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: 81 percent / BH3*SMe2 / chlorobenzene / 21 h / 80 - 130 °C
2: NaOtBu; Pd(OAc)2; [HP-t-Bu3][BF4] / toluene / 3 h / 160 °C / microwave irradiation
3: 35.5 percent / NaOtBu; Pd(OAc)2; [HP-t-Bu3][BF4] / dioxane / 18 h / Heating
View Scheme
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: 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
1: 81 percent / BH3*SMe2 / chlorobenzene / 21 h / 80 - 130 °C
2: NaOtBu; Pd(OAc)2; [HP-t-Bu3][BF4] / toluene / 3 h / 160 °C / microwave irradiation
View Scheme
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: 81 percent / BH3*SMe2 / chlorobenzene / 21 h / 80 - 130 °C
2: NaOtBu; Pd(OAc)2; [HP-t-Bu3][BF4] / toluene / 3 h / 160 °C / microwave irradiation
View Scheme
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: With triethylamine in DMF (N,N-dimethyl-formamide)
2: With chloroformic acid ethyl ester in DMF (N,N-dimethyl-formamide); toluene
Product distribution / selectivity;
参考文献
ALIZYME THERAPEUTICS LIMITED
Patent: WO2005/23808 A2, 2005 ;
Location in patent: Page/Page column 39 ;
反应条件
in tetrahydrofuran
0.666667 h;
参考文献
Elz; Keller
Archiv der Pharmazie, 1995 , vol. 328, # 7-8 p. 585 - 594
