4-FLUORO-BENZENESULFONYL-VAL-LEU-ALDEHYDE合成路线 （共 8 条）
反应条件
sulfur trioxide pyridine complex; N-ethyl-N,N-diisopropylamine in dichloromethane; dimethyl sulfoxide T=20°C; 0.666667 h;
参考文献
Senju Pharmaceutical Co., Ltd.
Patent: EP1557407 A1, 2005 ;
Location in patent: Page/Page column 6 ;
反应条件
diisobutylaluminium hydride in dichloromethane T=-78°C; 3 h;
参考文献
Payne, Richard J.; Brown, Karina M.; Coxon, James M.; Morton, James D.; Lee, Hannah Yun-Young; Abell, Andrew D.
Australian Journal of Chemistry, 2004 , vol. 57, # 9 p. 877 - 884
反应条件
1: 95 percent / iPr2NEt / CH2Cl2 / 4 h / Heating 2: 97 percent / KOH / H2O; tetrahydrofuran / 3 h / 40 °C 3: 89 percent / BOP; iPr2NEt / CH2Cl2 / 24 h 4: 73 percent / DIBALH / CH2Cl2 / 3 h / -78 °C View Scheme
参考文献
Inoue, Jun; Nakamura, Masayuki; Cui, Ying-She; Sakai, Yusuke; Sakai, Osamu; Hill, Jeanette R.; Wang, Kevin K. W.; Yuen, Po-Wai
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 868 - 871
反应条件
1: 89 percent / BOP; iPr2NEt / CH2Cl2 / 24 h 2: 73 percent / DIBALH / CH2Cl2 / 3 h / -78 °C View Scheme
参考文献
Inoue, Jun; Nakamura, Masayuki; Cui, Ying-She; Sakai, Yusuke; Sakai, Osamu; Hill, Jeanette R.; Wang, Kevin K. W.; Yuen, Po-Wai
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 868 - 871
反应条件
1: 76 percent / 1M NaOH / tetrahydrofuran; H2O / 18 h / 20 °C 2: 94 percent / RDC*HCl / tetrahydrofuran; CH2Cl2 / 18 h / 20 °C 3: 98 percent / ethyl acetate / 18 h / 20 °C 4: 37 percent / DIPEA; SO3*pyridine / dimethylsulfoxide; CH2Cl2 / 0.5 h / 0 °C View Scheme
参考文献
Inoue, Jun; Nakamura, Masayuki; Cui, Ying-She; Sakai, Yusuke; Sakai, Osamu; Hill, Jeanette R.; Wang, Kevin K. W.; Yuen, Po-Wai
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 868 - 871
反应条件
1: 98 percent / ethyl acetate / 18 h / 20 °C 2: 37 percent / DIPEA; SO3*pyridine / dimethylsulfoxide; CH2Cl2 / 0.5 h / 0 °C View Scheme
参考文献
Inoue, Jun; Nakamura, Masayuki; Cui, Ying-She; Sakai, Yusuke; Sakai, Osamu; Hill, Jeanette R.; Wang, Kevin K. W.; Yuen, Po-Wai
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 868 - 871
反应条件
1: 97 percent / KOH / H2O; tetrahydrofuran / 3 h / 40 °C 2: 89 percent / BOP; iPr2NEt / CH2Cl2 / 24 h 3: 73 percent / DIBALH / CH2Cl2 / 3 h / -78 °C View Scheme
参考文献
Payne, Richard J.; Brown, Karina M.; Coxon, James M.; Morton, James D.; Lee, Hannah Yun-Young; Abell, Andrew D.
Australian Journal of Chemistry, 2004 , vol. 57, # 9 p. 877 - 884
反应条件
1: 95 percent / iPr2NEt / CH2Cl2 / 4 h / Heating 2: 97 percent / KOH / H2O; tetrahydrofuran / 3 h / 40 °C 3: 89 percent / BOP; iPr2NEt / CH2Cl2 / 24 h 4: 73 percent / DIBALH / CH2Cl2 / 3 h / -78 °C View Scheme
参考文献
Payne, Richard J.; Brown, Karina M.; Coxon, James M.; Morton, James D.; Lee, Hannah Yun-Young; Abell, Andrew D.
Australian Journal of Chemistry, 2004 , vol. 57, # 9 p. 877 - 884
