(R)-4-(2-氟-4-(5-(羟基甲基)-2-氧代噁唑啉-3-基)苯基)哌嗪-1-羧酸叔丁酯合成路线 （共 6 条）
反应条件
1: With n-butyllithium in tetrahydrofuran T=-78°C; 0.5 h; 2: With (-)-(R)-glycidyl butyrate
参考文献
Orchid Chemicals & Pharmaceuticals Ltd
Patent: WO2004/18439 A1, 2004 ;
Location in patent: Page 32 ;
反应条件
1: tert-butyl 4-(4-(benzyloxycarbonyl)-2-fluorophenyl)piperazine-1-carboxylate With n-butyllithium in tetrahydrofuran T=-78°C; 0.333333 h; Inert atmosphere; 2: (-)-(R)-glycidyl butyrate in tetrahydrofuran T=-78 - 20°C; Inert atmosphere;
参考文献
Yan, Shanshan; Miller, Marvin J.; Wencewicz, Timothy A.; Moellmann, Ute
Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 1302 - 1305
反应条件
1.1: NaHCO3 / tetrahydrofuran 2.1: n-BuLi / tetrahydrofuran / 1.5 h / -78 °C 2.2: tetrahydrofuran View Scheme
参考文献
Roehrig, Susanne; Straub, Alexander; Pohlmann, Jens; Lampe, Thomas; Pernerstorfer, Josef; Schlemmer, Karl-Heinz; Reinemer, Peter; Perzborn, Elisabeth
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5900 - 5908
反应条件
1.1: H2 / Pd/C / methanol / 20 °C / 2844.31 Torr 2.1: NaHCO3 / tetrahydrofuran 3.1: n-BuLi / tetrahydrofuran / 1.5 h / -78 °C 3.2: tetrahydrofuran View Scheme
参考文献
Das, Biswajit; Rudra, Sonali; Yadav, Ajay; Ray, Abhijit; Raja Rao; Srinivas; Soni, Ajay; Saini, Suman; Shukla, Shalini; Pandya, Manisha; Bhateja, Pragya; Malhotra, Sunita; Mathur, Tarun; Arora; Rattan, Ashok; Mehta, Anita
Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 19 p. 4261 - 4267
反应条件
1.1: N-ethyldiisopropylamine / acetonitrile / 80 °C 2.1: TEA / CH2Cl2 / 0 - 20 °C 3.1: H2 / Pd/C / methanol / 20 °C / 2844.31 Torr 4.1: NaHCO3 / tetrahydrofuran 5.1: n-BuLi / tetrahydrofuran / 1.5 h / -78 °C 5.2: tetrahydrofuran View Scheme
参考文献
Das, Biswajit; Rudra, Sonali; Yadav, Ajay; Ray, Abhijit; Raja Rao; Srinivas; Soni, Ajay; Saini, Suman; Shukla, Shalini; Pandya, Manisha; Bhateja, Pragya; Malhotra, Sunita; Mathur, Tarun; Arora; Rattan, Ashok; Mehta, Anita
Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 19 p. 4261 - 4267
反应条件
1.1: TEA / CH2Cl2 / 0 - 20 °C 2.1: H2 / Pd/C / methanol / 20 °C / 2844.31 Torr 3.1: NaHCO3 / tetrahydrofuran 4.1: n-BuLi / tetrahydrofuran / 1.5 h / -78 °C 4.2: tetrahydrofuran View Scheme
参考文献
Das, Biswajit; Rudra, Sonali; Yadav, Ajay; Ray, Abhijit; Raja Rao; Srinivas; Soni, Ajay; Saini, Suman; Shukla, Shalini; Pandya, Manisha; Bhateja, Pragya; Malhotra, Sunita; Mathur, Tarun; Arora; Rattan, Ashok; Mehta, Anita
Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 19 p. 4261 - 4267
