反应条件
1: DIBAL-H / toluene; tetrahydrofuran / 45 °C 2: Et3N / toluene; tetrahydrofuran / 1 h / 45 °C 3: 65 percent / N-bromosuccinimide, H2O / dimethylsulfoxide / 0.17 h / 20 - 30 °C 4: H2O / ethanol / 3 h / Heating 6: 4.62 g / diethyl azodicarboxylate, Ph3P / tetrahydrofuran / 0.67 h 7: 3.45 g / H2 / 10percent Pd/C / ethanol / 1 h 8: 3.68 g / Na2CO3 / dimethylformamide / 1 h 9: 1.) sec-butyllithium, 2.) tosyl azide / 1.) cyclohexane, THF, -78 deg C, 15 min, 2.) cyclohexane, THF, RT, 1 h 10: 1.97 g / H2 / 10percent Pd/C / ethanol / 0.75 h / 2585.7 Torr 11: 1.26 g / t-BuOK / tetrahydrofuran / Ambient temperature 12: 0.48 g / H2 / 10percent Pd/C / ethanol / 18 h / 2585.7 Torr View Scheme
参考文献
Heier, Richard F.; Dolak, Lester A.; Duncan, J. Neil; Hyslop, Deborah K.; Lipton, Michael F.; Martin, Iain J.; Mauragis, Michael A.; Piercey, Montford F.; Nichols, Nanette F.; Schreur, Peggy J. K. D.; Smith, Martin W.; Moon, Malcolm W.
Journal of Medicinal Chemistry, 1997 , vol. 40, # 5 p. 639 - 646
