反应条件
1: 90 percent / K2CO3 / acetone / 4 h / Heating 2: 100 percent / NaH / tetrahydrofuran / 2 h / 0 °C 3: 100 percent / H2 / 10percent Pd/C / ethanol / 760 Torr / Ambient temperature 4: Et3N / CH2Cl2 / 1 h 5: CH2Cl2 / 1 h 6: 86 percent / anisole, TiCl4 / CH2Cl2 / 1 h / 0 °C 7: 93 percent / γ-collidine / dimethylformamide / 1.5 h / 65 °C 8: 98 percent / Et3N / toluene / 5 h / Ambient temperature 9: 1.) NaH, 2.) benzyl bromide / 1.) THF, toluene, -20 deg C, 1 h, 2.) THF, toluene, -20 deg C, 2 h 10: DBU / toluene; tetrahydrofuran / 2 h 11: 89 percent / phosphate buffer pH 3 / 2.5 h / Ambient temperature View Scheme
参考文献
ORCHID CHEMICALS AND PHARMACEUTICALS LIMITED; KARALE, Sanjay Nivrutti; JANGALE, Arvind Atamaram; KALDATE, Ram Dattatraya
Patent: WO2011/141847 A1, 2011 ;