4-溴-2-甲基-6-甲氧基苯胺合成路线 （共 5 条）
反应条件
(benzyl)-tri-(methyl)-ammonium bromide; calcium carbonate in methanol; dichloromethane T=20°C; 1 h;
参考文献
Hartmann, Rolf; Frotscher, Martin; Oberwinkler, Sandrine; Ziegler, Erika; Messinger, Josef; Thole, Heinrich-Hubert
Patent: US2010/204234 A1, 2010 ;
Location in patent: Page/Page column 13 ;
US 20100204234 A1
反应条件
1: With hydrogenchloride; sodium nitrite in water; acetic acid T=0°C; 0.5 h; 2: With hypophosphorous ether in water; acetic acid T=0 - 20°C;
参考文献
GILEAD SCIENCES, INC.; KOREAN RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Patent: WO2009/5674 A2, 2009 ;
Location in patent: Page/Page column 423 ;
反应条件
1.1: hydrogenchloride; sodium nitrite / water / 0.5 h / 0 °C 1.3: 4 h / 0 - 50 °C 2.1: diisobutylaluminium hydride / toluene; tetrahydrofuran / -78 - 20 °C 2.2: 0 - 20 °C View Scheme
反应条件
1.1: NaNO2; aq. HCl / acetic acid / 0.75 h / 0 °C
1.2: 85 percent / aq. hypophosphorous acid / 0 - 20 °C
2.1: n-BuLi / tetrahydrofuran; hexane / 2 h / -78 °C
2.2: tetrahydrofuran; hexane / -78 - 20 °C
3.1: 1.494 g / aq. HCl / tetrahydrofuran / 2 h / 20 °C
View Scheme
参考文献
SMITHKLINE BEECHAM CORPORATION; VITAE PHARMACEUTICALS, INC.
Patent: WO2008/124582 A1, 2008 ;
WO 2008/124582 A1
反应条件
1.1: hydrogenchloride; sodium nitrite / water / 0.5 h / 0 °C
1.3: 4 h / 0 - 50 °C
2.1: diisobutylaluminium hydride / toluene; tetrahydrofuran / -78 - 20 °C
2.2: 0 - 20 °C
3.1: 2-methyl-but-2-ene; water; sodium chlorite; sodium dihydrogenphosphate / tert-butyl alcohol / 0.5 h / 20 °C
3.2: pH 1
View Scheme
参考文献
TETRAPHASE PHARMACEUTICALS, INC.; XIAO, Xiao-yi; CLARK, Roger; HUNT, Diana; ROeNN, Magnus; PLAMONDON, Louis; HE, Minsheng; SUTCLIFFE, Joyce; GROSSMAN, Trudy
Patent: WO2011/123536 A1, 2011 ;
