反应条件
1: 1.) n-BuLi / 1.) THF, hexane, -78 deg C, 5 min, 2.) THF, hexane, from -78 deg C to RT, 30 min 2: 1.) dibutylboron triflate, diisopropylethylamine, 3.) 30percent aq. H2O2 3: 1.) diisopropylethylamine, dibutylboron triflate, 2.) lithium borohydride, 3.) 30percent aq. H2O2 4: 1.) camphorsulfonic acid, 2.) acetone / 1.) CH2Cl2, RT, 45 min, 2.) CH2Cl2, RT, overnight 5: 91 percent / periodic acid, RuCl3*3H2O / acetonitrile; CCl4; H2O / 2 h / Ambient temperature 6: Et3N, diethylphosphoryl cyanide / CH2Cl2 / 2 h / Ambient temperature 7: acetyl chloride / methanol / 14 h / Ambient temperature 8: Et3N, diethylphosphoryl cyanide / CH2Cl2 / 14 h 9: trifluoroacetic acid / CH2Cl2 / 0.5 h / Ambient temperature 10: Et3N, diethylphosphoryl cyanide / CH2Cl2 / 14 h 11: 1-hydroxybenzotriazole / methanol / 14 h / Ambient temperature View Scheme
参考文献
Thaisrivongs, Suvit; Pals, Donald T.; Kroll, Lisa T.; Turner, Steve R.; Han, Fu-Son
Journal of Medicinal Chemistry, 1987 , vol. 30, # 6 p. 976 - 982