(AlphaS,γS)- Alpha-[[(叔丁氧基)羰基]氨基]-4-甲氧基-3-(3-甲氧基丙氧基)- γ-异丙基苯戊酸甲酯合成路线 (共 14 条)
反应条件
1.1: BuLi / hexane / 0.5 h / -75 °C
1.2: 91 percent / tetrahydrofuran / 20 h / -75 - -20 °C
2.1: 90 percent / 1N HCl / acetonitrile / 1.5 h / 20 °C
3.1: 82 percent / Et3N / CH2Cl2 / 20 h / 20 °C
View Scheme
参考文献
Goeschke, Richard; Stutz, Stefan; Heinzelmann, Walter; Maibaum, Juergen
Helvetica Chimica Acta, 2003 , vol. 86, # 8 p. 2848 - 2870
反应条件
1.1: 94 percent / H2O2; LiOH / tetrahydrofuran; H2O / 3 h / 20 °C
2.1: NaBH4 / tetrahydrofuran / 0.75 h / 20 °C
2.2: 90 percent / I2 / tetrahydrofuran / 96 h / 20 °C
3.1: 97 percent / NBS; Ph3P / CH2Cl2 / 18 h / 20 °C
4.1: BuLi / hexane / 0.5 h / -75 °C
4.2: 91 percent / tetrahydrofuran / 20 h / -75 - -20 °C
5.1: 90 percent / 1N HCl / acetonitrile / 1.5 h / 20 °C
6.1: 82 percent / Et3N / CH2Cl2 / 20 h / 20 °C
View Scheme
参考文献
Goeschke, Richard; Stutz, Stefan; Heinzelmann, Walter; Maibaum, Juergen
Helvetica Chimica Acta, 2003 , vol. 86, # 8 p. 2848 - 2870
反应条件
1: 70 percent / 1N HCl / acetonitrile / 1.5 h / 20 °C
2: Huenig's base / CH2Cl2 / 16 h / 20 °C
View Scheme
参考文献
Goeschke, Richard; Stutz, Stefan; Heinzelmann, Walter; Maibaum, Juergen
Helvetica Chimica Acta, 2003 , vol. 86, # 8 p. 2848 - 2870
反应条件
1: With lithium borohydride in tetrahydrofuran
T=20°C; 15 h;
2: With hydrogenchloride in tetrahydrofuran; water; ethyl acetate
参考文献
VITAE PHARMACEUTICALS, INC.
Patent: WO2007/123718 A1, 2007 ;
Location in patent: Example 3 ;
WO 2007/123718 A1