N-叔丁氧羰基-1,2-乙二胺合成路线 （共 68 条）
反应条件
1: With sodium tris(acetoxy)borohydride in tetrahydrofuran
T=20°C;
2: With methanol in tetrahydrofuran
T=70°C; 1.5 h;
参考文献
sanofi-aventis
Patent: US2008/269170 A1, 2008 ;
Location in patent: Page/Page column 28 ;
反应条件
1: With sodium tris(acetoxy)borohydride; acetic acid in 1,2-dichloro-ethane
T=20°C; 0.5 h;
2: With sodium hydrogencarbonate in water; 1,2-dichloro-ethane
3: With ammonium chloride; lithium hexamethyldisilazane
more than 3 stages;
参考文献
AMGEN INC.
Patent: WO2009/78992 A1, 2009 ;
Location in patent: Page/Page column 42-43 ;
WO 2009/078992 A1
反应条件
potassium carbonate in chloroform; acetonitrile
参考文献
Fader; Boyd; Tsantrizos
Journal of Organic Chemistry, 2001 , vol. 66, # 10 p. 3372 - 3379
反应条件
1: in dichloromethane
T=0°C; 1 h; Inert atmosphereMolecular sieve;
2: With palladium 10 on activated carbon; hydrogen in dichloromethane
P=2585.81 Torr; 4 h; Inert atmosphereMolecular sieve;
参考文献
Cooper, Daniel C.; Suggs, J. William
Tetrahedron Letters, 2012 , vol. 53, # 51 p. 6943 - 6945
反应条件
triethylamine in dichloromethane
T=20°C; 4 h;
参考文献
LG LIFE SCIENCES LTD.; YAMANOUCHI PHARMACEUTICAL CO., LTD.
Patent: WO2005/47253 A1, 2005 ;
Location in patent: Page/Page column 55 ;
WO 2005/047253 A1
反应条件
triethylamine in toluene
Substitution; 8 h; Heating;
参考文献
AMGEN, INC.
Patent: WO2006/66172 A1, 2006 ;
Location in patent: Page/Page column 25 ;
WO 2006/066172 A1
反应条件
1: 5.2 g / K2CO3 / dimethylformamide / 70 °C
2: 2.75 g / ammonium formate / 10percent Pd/C / ethanol / 70 °C
View Scheme
参考文献
PRINCIPIA BIOPHARMA INC.; BRAMELD, Kenneth, A.; OWENS, Tim, A.
Patent: WO2014/36016 A1, 2014 ;
反应条件
1.1: methanol / 20 °C / Molecular sieve
1.2: 16 h / -10 - 20 °C
2.1: triethylamine / chloroform / 16 h / 5 - 20 °C / Sealed tube
View Scheme
参考文献
PHARMACOFORE, INC.; JENKINS, Thomas, E.; HUSFELD, Craig, O.; SEROOGY, Julie, D.; WRAY, Jonathan, W.
Patent: WO2011/133150 A1, 2011 ;
反应条件
triethylamine in dichloromethane
T=60°C; 0.416667 h; Microwave irradiation;
参考文献
Weiss, Stefan; Keller, Max; Bernhardt, Guenther; Buschauer, Armin; Koenig, Burkhard
Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 17 p. 6292 - 6304
反应条件
1.1: molecular sieves 3 Angstroem / methanol / 4 h / 20 °C
1.2: 61 percent / NaBH4 / methanol / 16 h / -5 °C
2.1: 90 percent / DIEA / dimethylformamide / 0 - 20 °C
3.1: 70 percent / ammonium formate / Pd/C / methanol / 16 h / Heating
View Scheme
参考文献
Muller, Dan; Zeltser, Irena; Bitan, Gal; Gilon, Chaim
Journal of Organic Chemistry, 1997 , vol. 62, # 2 p. 411 - 416
