反应条件
1: 60 percent / H2, AcCl / 5percent Pd/C / ethanol / 5 h / 760 Torr / Ambient temperature 2: 24 percent / Et3N / ethanol 3: 62 percent / K2CO3 / dimethylformamide / 16 h / Ambient temperature 4: 98 percent / trifluoroacetic acid / CH2Cl2 / 16 h / Ambient temperature 5: 100 percent / Et3N / CH2Cl2 / 0.75 h / -70 °C 6: 95 percent / aq. NaOH / methanol / 3 h / 50 °C 7: 1.) CDI, 2.) NH3 / 1.) THF, RT, 3 h, 2.) THF, EtOH, a.) RT, 16 h, b.) reflux, 4 h View Scheme
参考文献
Judd; Dowle; Middlemiss; Scopes; Ross; Jack; Pass; Tranquillini; Hobson; Panchal; Stuart; Paton; Hubbard; Hilditch; Drew; Robertson; Clark; Travers; Hunt; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 19 p. 3108 - 3120