2,3-二氢-n-2-丙炔-1-基-1H-茚-1-胺合成路线 (共 12 条)
反应条件
methanol; sodium tetrahydroborate T=0 - 35°C;
参考文献
WO2010/59913 A2, ;
Page/Page column 16-17 ;
反应条件
1: With sodium tetrahydroborate; acetic acid in tetrahydrofuran T=30 - 35°C; Inert atmosphere; 2: With potassium carbonate in tetrahydrofuran; water T=20 - 25°C; pH=7 - 8;
参考文献
DIPHARMA FRANCIS S.r.I.
Patent: US2010/29987 A1, 2010 ;
Location in patent: Page/Page column 3-4 ;
反应条件
sodium hydroxide in water; toluene T=20 - 47°C; 4.95 h; Inert atmosphereIndustry scale; Product distribution / selectivity;
参考文献
Frenkel, Anton; Lidor-Hadas, Ramy; Bahar, Eliezer
Patent: US2011/152381 A1, 2011 ;
Location in patent: Page/Page column 8-9 ;
反应条件
1: With methanol; sodium tetrahydroborate T=25 - 35°C; 2: With acetic acid in methanol; water 0.166667 h; 3: With sodium hydroxide in methanol; water pH=12;
参考文献
WO2010/59913 A2, ;
Page/Page column 17-18 ;
反应条件
1: in methanol T=20°C; 0.5 h; 2: With sodium acetate; sodium cyanoborohydride in methanol Reflux; Product distribution / selectivity;
参考文献
DR. REDDY'S LABORATORIES LTD.; DR. REDDY'S LABORATORIES, INC.
Patent: US2011/218360 A1, 2011 ;
Location in patent: Page/Page column 7 ;
反应条件
potassium carbonate in acetonitrile T=55°C; 24 h;
参考文献
WO2011/48612 A2, ;
Page/Page column 22 ;
反应条件
potassium carbonate; N,N-dimethyl-formamide; sodium hydroxide T=40 - 70°C; 7 h;
参考文献
WO2012/153349 A2, ;
Page/Page column 30 ;
反应条件
1: ethanol / 8 h / 25 - 30 °C 2: ethanol; sodium tetrahydroborate / 8 h / 25 - 30 °C View Scheme
反应条件
1: hydrogen; ammonia / Raney nickel / methanol / 10 - 42 °C / Autoclave 2: potassium carbonate; N,N-dimethyl-formamide; sodium hydroxide / 7 h / 40 - 70 °C View Scheme
反应条件
Chiralcel-OJ-H (4-methylbenzoate cellulose coated on silica) column in ethanol; hexane; diethylamine; isopropyl alcohol T=27°C; Resolution of racemate; TemperatureSolvent;
参考文献
Chirality, , vol. 25, # 6 p. 324 - 327