4-溴-1,2-亚甲二氧基苯合成路线 （共 128 条）
反应条件
1: 1) 9-BBN, 2) CH3ONa / 2) dichloro<1,1'-bis(diphenylphosphino)ferrocene>palladium(II) / 1) THF, room temperature, 3 h, 2) THF, reflux, 5 h
2: 94 percent / KOH / ethanol / 2 h / Ambient temperature
3: 87 percent / polyphosphonate ester / CHCl3; diethyl ether / 5 h / Ambient temperature
View Scheme
参考文献
Thibonnet, Jerome; Abarbri, Mohamed; Parrain, Jean-Luc; Duchene, Alain
Tetrahedron Letters, 1996 , vol. 37, # 42 p. 7507 - 7510
反应条件
1: 1) 9-BBN, 2) CH3ONa / 2) dichloro<1,1'-bis(diphenylphosphino)ferrocene>palladium(II) / 1) THF, room temperature, 3 h, 2) THF, reflux, 5 h
2: 94 percent / KOH / ethanol / 2 h / Ambient temperature
View Scheme
参考文献
Esteban, Gemma; Lopez-Sanchez, Miguel A.; Martinez, Ma. Eugenia; Plumet, Joaquin
Tetrahedron, 1998 , vol. 54, # 1-2 p. 197 - 212
反应条件
sodium t-butanolate; palladium diacetate; tri-tert-butyl phosphine in o-xylene
T=120°C; Yield given;
参考文献
Nishiyama, Masakazu; Yamamoto, Toshihide; Koie, Yasuyuki
Tetrahedron Letters, 1998 , vol. 39, # 7 p. 617 - 620
反应条件
NiCl2((PPh3)P)2 in 1,4-dioxane
1 h; Heating;
参考文献
Trost, Barry M.; Yoshida, Jun-ichi
Tetrahedron Letters, 1983 , vol. 24, # 45 p. 4895 - 4898
反应条件
hydrogenchloride; hydrogen sulfide in tetrahydrofuran
参考文献
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Patent: US6057369 A1, 2000 ;
US 6057369 A
反应条件
magnesium in tetrahydrofuran
1.) reflux, 30 min, 2.) -45 deg C, 1.5 h; room temperature, 1.5 h;
参考文献
Hitotsuyanagi, Yukio; Kobayashi, Masatsugu; Takeya, Koichi; Itokawa, Hideji
Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), 1995 , # 11 p. 1387 - 1390
反应条件
1: 1,2-methylenedioxy-4-bromobenzene With n-butyllithium in tetrahydrofuran; hexanes
T=-78°C; 0.5 h;
2: diethyl disulphide in tetrahydrofuran; hexanes
0.5 h;
参考文献
CRYSTAX PHARMACEUTICALS, S.L.
Patent: WO2009/7399 A1, 2009 ;
Location in patent: Page/Page column 88-89 ;
反应条件
1: 90 percent / n-BuLi; BF3*Et2O / hexane; tetrahydrofuran / 0.08 h / -78 °C
2: 98 percent / PCC; silica gel / CH2Cl2 / 6 h / 20 °C
View Scheme
参考文献
Gao, Shuanhu; Tu, Yong Qiang; Song, Zhenlei; Wang, Aixia; Fan, Xiaohui; Jiang, Yijun
Journal of Organic Chemistry, 2005 , vol. 70, # 16 p. 6523 - 6525
