N-Boc-2-哌啶乙酸甲酯合成路线 (共 24 条)
反应条件
1: (2S)-1-tert-butoxycarbonyl-2-carboxymethylpiperidine With O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate; N-ethyl-N,N-diisopropylamine in N,N-dimethyl-formamide T=20°C; 0.333333 h; 2: methanol in N,N-dimethyl-formamide T=20°C; 0.5 h;
参考文献
GLAXO GROUP LIMITED; ALVARO, Giuseppe; AMANTINI, David; BELVEDERE, Sandro
Patent: WO2010/60471 A1, 2010 ;
Location in patent: Page/Page column 15-16 ;
WO 2010/060471 A1
反应条件
hydrogen; palladium dihydroxide in ethyl acetate T=20°C; P=760 Torr;
参考文献
Calvet-Vitale, Sandrine; Vanucci-Bacque, Corinne; Fargeau-Bellassoued, Marie-Claude; Lhommet, Gerard
Tetrahedron, 2005 , vol. 61, # 32 p. 7774 - 7782
反应条件
1: (S)-(-)-1-(tert-butoxycarbonyl)-2-piperidine carboxylic acid With 4-methyl-morpholine; isobutyl chloroformate in tetrahydrofuran T=-30°C; 1 h; 2: diazomethane in tetrahydrofuran; diethyl ether T=-30 - 20°C; 16 h; 3: methanol With silver benzoate T=20°C; 16 h; Cooling with ice;
参考文献
ENDO PHARMACEUTICALS INC.; GUPTA, Sandeep; PRIESTLEY, Tony; LAPING, Nicholas, James
Patent: WO2014/28675 A1, 2014 ;
Location in patent: Page/Page column 100-101 ;
反应条件
hydrogen; palladium on activated charcoal in methanol
参考文献
Gray, Diane; Concellon, Carmen; Gallagher, Timothy
Journal of Organic Chemistry, 2004 , vol. 69, # 14 p. 4849 - 4851
反应条件
silver benzoate T=0 - 20°C; 3 h; Inert atmosphere;
参考文献
Hanessian, Stephen; Chattopadhyay, Amit Kumar
Organic Letters, 2014 , vol. 16, # 1 p. 232 - 235
反应条件
silver benzoate in methanol; ethyl acetate; triethylamine
参考文献
US6147088 A1, ;
US 6147088 A
US6150352 A1, ;
US 6150352 A
反应条件
1.1: Et3N / tetrahydrofuran; diethyl ether / 1 h / 0 °C 2.1: diethyl ether / 3 h / 0 °C 2.2: AgOBz; Et3N / 3 h / 0 - 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 9, # 17 p. 2621 - 2624
反应条件
4-(N,N-dimethlyamino)pyridine; dicyclohexyl-carbodiimide in diethyl ether Ambient temperature;
参考文献
Morley, Christopher; Knight, David W.; Share, Andrew C.
Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), 1994 , # 20 p. 2903 - 2908
反应条件
1: 67 percent / H2 / PtO2 / methanol / 24 h / 20 °C / 760 Torr 2: 84 percent / H2 / Pd(OH)2/C / ethyl acetate / 20 °C / 760 Torr View Scheme
参考文献
Tetrahedron, , vol. 61, # 32 p. 7774 - 7782
反应条件
1: 82 percent / HC(OMe)3; p-TSA / 6 h / 20 °C 2: NaI; Na2CO3; tetrabutylammonium iodide / acetonitrile / Heating 3: 67 percent / BF3*Et2O / CH2Cl2 / 0 °C 4: 63 percent / NaBH(OAc)3 / acetic acid; acetonitrile / 52 h / 0 - 20 °C 5: H2 / Pd(OH)2/C / methanol / 4 h / 20 °C / 760 Torr 6: 0.19 g / NEt3 / CH2Cl2 / 15 h / 20 °C View Scheme
参考文献
Tetrahedron, , vol. 59, # 33 p. 6333 - 6339