N-Boc-4,4-二氟-L-脯氨酸合成路线 （共 8 条）
反应条件
1: With water; sodium hydroxide in tetrahydrofuran; methanol T=20°C; 1 h; 2: With hydrogenchloride in water
参考文献
ALMIRALL, S.A.; BERNAL ANCHUELA, Francisco Javier; CARRASCAL RIERA, Marta; CATURLA JAVALOYES, Juan Francisco; GRACIA FERRER, Jordi; MATASSA, Victor Giulio; TERRICABRAS BELART, Emma; TALTAVULL MOLL, Joan; ERRA SOLA, Montserrat
Patent: WO2012/146666 A1, 2012 ;
Location in patent: Page/Page column 138-139 ;
WO 2012/146666 A1
反应条件
1: 72 percent / DAST / CH2Cl2 / -78 - 20 °C 2: 92 percent / aq. NaOH / tetrahydrofuran / 1 h View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 14, # 8 p. 2725 - 2746
反应条件
1: 57 percent / PDC / CH2Cl2 / 72 h 2: 72 percent / DAST / CH2Cl2 / -78 - 20 °C 3: 92 percent / aq. NaOH / tetrahydrofuran / 1 h View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 14, # 8 p. 2725 - 2746
反应条件
1: 95 percent / Et3N / CH2Cl2 / Ambient temperature 2: 81 percent / PDC, 3 Angstroem molecular sieves / CH2Cl2 / Ambient temperature 3: 89 percent / DAST / CH2Cl2 / -78 deg C to r.t. 4: 95 percent / LiOH / acetonitrile; H2O / Ambient temperature View Scheme
参考文献
Tetrahedron Letters, , vol. 39, # 10 p. 1169 - 1172
反应条件
1: 95 percent / Et3N / CH2Cl2 / Ambient temperature 2: 81 percent / PDC, 3 Angstroem molecular sieves / CH2Cl2 / Ambient temperature 3: 89 percent / DAST / CH2Cl2 / -78 deg C to r.t. 4: 95 percent / LiOH / acetonitrile; H2O / Ambient temperature View Scheme
参考文献
Tetrahedron Letters, , vol. 39, # 10 p. 1169 - 1172
反应条件
1: With 4-methyl-morpholine; isobutyl chloroformate in tetrahydrofuran T=-10°C; 0.75 h; 2: With sodium tetrahydroborate in tetrahydrofuran; water T=0°C; 2 h; 3: With ammonium chloride in tetrahydrofuran; water T=20°C;
参考文献
Bristol-Myers Squibb Company
Patent: US2011/82165 A1, 2011 ;
Location in patent: Page/Page column 29-30 ;
反应条件
1: With pivaloyl chloride; triethylamine in dichloromethane
T=-15°C; 1 h;
2: With ammonia in dichloromethane; water
T=-15°C; 1 h;
参考文献
SANOFI-SYNTHELABO
Patent: WO2003/74500 A2, 2003 ;
Location in patent: Page/Page column 15-16 ;
反应条件
hydrogenchloride in 1,4-dioxane; methanol
T=20°C; 6 h;
参考文献
Bristol-Myers Squibb Company
Patent: US2008/9497 A1, 2008 ;
Location in patent: Page/Page column 109 ;
US 20080009497 A1
