反应条件
1: 1.) n-BuLi, TMEDA, 2.) triisopropyl borate, 3.) tetrakis(triphenylphosphine)palladium, Na2CO3 2: 100 percent / Br2 / CCl4 / 0.67 h / 0 - 5 °C 3: 92 percent / aq. NaOH / methanol / 3 h / Heating 4: 18 percent / diphenylphosphorazidate, Et3N / dioxane / 20 h / Heating 5: 97 percent / NBS, benzoyl peroxide / CCl4 / 1.5 h / Heating; Irradiation 6: 62 percent / K2CO3 / dimethylformamide / 16 h / Ambient temperature 7: 98 percent / trifluoroacetic acid / CH2Cl2 / 16 h / Ambient temperature 8: 100 percent / Et3N / CH2Cl2 / 0.75 h / -70 °C 9: 95 percent / aq. NaOH / methanol / 3 h / 50 °C 10: 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
