N-Boc-4-亚甲基-L-脯氨酸合成路线 （共 18 条）
反应条件
1: Methyltriphenylphosphonium bromide With potassium tert-butylate in tetrahydrofuran T=0 - 20°C; 2 h; 2: (2S)-4-Oxo-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester in tetrahydrofuran T=0 - 20°C;
参考文献
ENANTA PHARMACEUTICALS, INC.; QIU, Yao-Ling; PENG, Xiaowen; KIM, In, Jong; CAO, Hui; TANG, Datong; OR, Yat, Sun; WANG, Guoqiang; XU, Guoyou
Patent: WO2012/158861 A2, 2012 ;
Location in patent: Page/Page column 19-20 ;
反应条件
potassium tert-butylate in 2-methyl tetrahydrofuran; isopropanol acetate
反应条件
sodium hydroxide in 1,4-dioxane; water T=25°C; 3 h;
参考文献
Manfre; Kern; Biellmann
Journal of Organic Chemistry, 1992 , vol. 57, # 7 p. 2060 - 2065
反应条件
1: 76 percent / Na-amalgam, K2HPO4 / methanol / 1) 0 deg to r.t., 2) r.t., 1 h 2: (C2H5)3N / tetrahydrofuran / 12 h / Ambient temperature View Scheme
参考文献
Tetrahedron, , vol. 48, # 31 p. 6529 - 6536
反应条件
1: 58 percent / AIBN, (n-Bu)3SnH / benzene / 10 h / Heating 2: 76 percent / Na-amalgam, K2HPO4 / methanol / 1) 0 deg to r.t., 2) r.t., 1 h 3: (C2H5)3N / tetrahydrofuran / 12 h / Ambient temperature View Scheme
参考文献
Tetrahedron, , vol. 48, # 31 p. 6529 - 6536
反应条件
1: 66 percent / 1) P(C6H5)3Br2 / CH2Cl2 / 4 h / 0 °C 2: 58 percent / AIBN, (n-Bu)3SnH / benzene / 10 h / Heating 3: 76 percent / Na-amalgam, K2HPO4 / methanol / 1) 0 deg to r.t., 2) r.t., 1 h 4: (C2H5)3N / tetrahydrofuran / 12 h / Ambient temperature View Scheme
参考文献
Tetrahedron, , vol. 48, # 31 p. 6529 - 6536
反应条件
triethylamine in tetrahydrofuran 12 h; Ambient temperature; Yield given;
参考文献
Tetrahedron, , vol. 48, # 31 p. 6529 - 6536
反应条件
sodium hydride 1.) 50 deg C, 4 h, THF; 2.) 50 deg C, THF, overnight; Yield given. Multistep reaction;
参考文献
Canadian Journal of Chemistry, , vol. 60, # 23 p. 2903 - 2907
反应条件
hydrogen; palladium 10 on activated carbon in isopropyl alcohol P=760.051 Torr; 18 h;
参考文献
BRISTOL-MYERS SQUIBB COMPANY; ROMINE, Jeffrey Lee
Patent: WO2012/18325 A1, 2012 ;
Location in patent: Page/Page column 146 ;
WO 2012/018325 A1
反应条件
1: With diethylzinc in n-heptane; dichloromethane T=-5 - 20°C; 19.5 h; 2: With lithium hydroxide hydrate; water in methanol T=15 - 25°C; 13.5 h; 3: With iodine; sodium hydrogencarbonate in water T=25°C; 40 h;
参考文献
US2013/324740 A1, ;
Paragraph 0131; 0132; 0133; 0135; 0136; 0137 ;
