反应条件
1: NaBH4 / tetrahydrofuran; H2O / 0.25 h / 0 °C 2: pyridine / 16 h / 20 °C 3: TsOH*H2O / ethanol / 1.) 20 deg C, 1 h, 2.) 4 deg C, overnight 4: 69 percent / t-BuOK / dimethylformamide / 1 h / 20 °C 5: 80 percent / dimethylformamide / 8.5 h / 120 °C 6: 1.) 33percent MeNH2, 2.) 4 M HCl / 1.) EtOH, r.t., 1 h, 2.) EtOH, EtOAc, r.t., overnight 7: 48 percent / 1-hydroxybenzotriazole hydrate, dicyclohexylcarbodiimide, N-ethylmorpholine / tetrahydrofuran / 64 h / Ambient temperature 8: H2 / 10percent Pd/C / ethanol / 16 h 9: 1-hydroxybenzotriazole hydrate, dicyclohexylcarbodiimide, N-ethylmorpholine / tetrahydrofuran / 16 h / Ambient temperature View Scheme
参考文献
Journal of Organic Chemistry, , vol. 59, # 13 p. 3656 - 3664
