1,2-二氢-2-氧代螺[4H-3,1-苯并恶嗪-4,4'-哌啶]-1'-羧酸叔丁酯合成路线 (共 4 条)
反应条件
1: phenyl-carbamic acid tert-butyl ester With tert.-butyl lithium in tetrahydrofuran; pentane T=-70 - -20°C; 2.5 h; 2: (4-oxo-cyclohexyl)-carbamic acid tert-butyl ester With potassium tert-butylate in tetrahydrofuran; pentane T=-70 - 20°C; 3: With hydrogenchloride in tetrahydrofuran; diethyl ether; water; pentane T=0°C; pH=7;
参考文献
WO2008/21375 A2, ;
Page/Page column 42-43 ;
WO 2008/021375 A2
反应条件
t-BuOK; tert.-butyl lithium 1.) pentane, THF, a) -70 deg, 0.5 h, b) -20 deg, 2.5 h, 2.) THF, a) from -70 deg to RT, 4 h, b) RT, 16 h; Yield given. Multistep reaction;
参考文献
Journal of Medicinal Chemistry, , vol. 26, # 5 p. 657 - 661
反应条件
trifluoroacetic acid in dichloromethane 1 h; Ambient temperature;
参考文献
Clark; Caroon; Kluge; Repke; Roszkowski; Strosberg; Baker; Bitter; Okada
Journal of Medicinal Chemistry, 1983 , vol. 26, # 5 p. 657 - 661
反应条件
1: 1.) NaH / 1.) DMF, 20 deg, 0.5 h, 2.) DMF, 20 deg, 1 h
2: 78 percent / trifluoroacetic acid / CH2Cl2 / 2 h / Ambient temperature
View Scheme
参考文献
Clark; Caroon; Kluge; Repke; Roszkowski; Strosberg; Baker; Bitter; Okada
Journal of Medicinal Chemistry, 1983 , vol. 26, # 5 p. 657 - 661