反式-4-氨基环己醇盐酸盐合成路线 （共 20 条）
反应条件
triethylamine in isopropyl alcohol T=0 - 60°C; 2.5 h;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2004/18480 A1, 2004 ;
Location in patent: Page 87-88 ;
WO 2004/018480 A1
反应条件
molecular sieves in tetrahydrofuran; sodium hydroxide; dichloromethane
参考文献
Bridger, Gary; Kaller, Al; Harwig, Curtis; Skerlj, Renato; Bogucki, David; Wilson, Trevor R.; Crawford, Jason; McEachern, Ernest J.; Atsma, Bem; Nan, Siqiao; Zhou, Yuanxi; Schols, Dominique; Smith, Christopher D.; Di Fluri, Maria R.
Patent: US2004/19058 A1, 2004 ;
US 20040019058 A1
反应条件
1: 93 percent / aq. NaOH / dioxane / 2 h / 20 °C 2: 98 percent / (COCl)2; Me2SO; Et3N / CH2Cl2 / 1.5 h / -78 - 20 °C View Scheme
参考文献
Noguchi, Hirohide; Aoyama, Toyohiko; Shioiri, Takayuki
Heterocycles, 2002 , vol. 58, p. 471 - 504
反应条件
iron sulphate heptahydrate; tert-butyl hydroperoxide; calcium carbonate in water; acetonitrile T=60°C; 16 h; Inert atmosphere;
参考文献
Ghosh, Subhash Chandra; Ngiam, Joyce S. Y.; Chai, Christina L. L.; Seayad, Abdul M.; Dang, Tuan Thanh; Chen, Anqi
Advanced Synthesis and Catalysis, 2012 , vol. 354, # 8 p. 1407 - 1412
反应条件
1: potassium carbonate / acetonitrile / 12 h / 20 - 30 °C / Inert atmosphere 2: Jone's reagent / acetone / 0.58 h / 20 - 30 °C / Cooling with ice; Inert atmosphere View Scheme
反应条件
1: KOH; Et3N / acetonitrile 2: 80 percent / PPh3; DEAD / tetrahydrofuran / 25 °C 3: sodium naphthalide / 1,2-dimethoxy-ethane / -35 - 25 °C View Scheme
参考文献
Cheng, Jie; Trudell, Mark L.
Organic Letters, 2001 , vol. 3, # 9 p. 1371 - 1373
反应条件
1.1: potassium carbonate / acetonitrile / 12 h / 20 - 30 °C / Inert atmosphere
2.1: Jone's reagent / acetone / 0.58 h / 20 - 30 °C / Cooling with ice; Inert atmosphere
3.1: sodium acetate; sodium tris(acetoxy)borohydride / acetonitrile / 12 h / 20 - 30 °C / pH 6 - 7 / Inert atmosphere
3.2: pH 8
4.1: hydrogen; acetic acid / palladium 10 on activated carbon / dichloromethane; methanol / 12 h / 20 - 30 °C / 2280.15 Torr / Inert atmosphere
View Scheme
参考文献
SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.; JIANGSU HENGRUI MEDICINE CO., LTD.
Patent: US2012/184543 A1, 2012 ;
反应条件
1.1: potassium carbonate / acetonitrile / 12 h / 20 - 30 °C / Inert atmosphere
2.1: Jone's reagent / acetone / 0.58 h / 20 - 30 °C / Cooling with ice; Inert atmosphere
3.1: sodium acetate; sodium tris(acetoxy)borohydride / acetonitrile / 12 h / 20 - 30 °C / pH 6 - 7
3.2: pH 8
4.1: hydrogen; acetic acid / palladium 10 on activated carbon / methanol / 12 h / 20 - 30 °C / 2280.15 Torr
View Scheme
参考文献
SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.; JIANGSU HENGRUI MEDICINE CO., LTD.
Patent: US2012/184543 A1, 2012 ;
反应条件
1: potassium carbonate / water / 1 h / 20 °C
2: 1H-imidazole / N,N-dimethyl-formamide; toluene / 40 °C / Cooling with ice
3: triethylsilane; BiBr3 / acetonitrile / 20 °C
4: hydrazine hydrate / ethanol / 1 h / 70 °C
View Scheme
参考文献
BRISTOL-MYERS SQUIBB COMPANY; MARKWALDER, Jay A.; FINK, Brian E.; GAVAI, Ashvinikumar V.; HE, Liqi; KIM, Soong-Hoon; SEITZ, Steven P.
Patent: WO2011/123493 A1, 2011 ;
WO 2011/123493 A1
反应条件
sodium methylate in 1,4-dioxane; methanol
参考文献
SANOFI-AVENTIS DEUTSCHLAND GMBH
Patent: WO2007/12422 A1, 2007 ;
Location in patent: Page/Page column 87-88 ;
WO 2007/012422 A1
