GNE 390; (S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-d]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮合成路线 (共 6 条)
反应条件
N-ethyl-N,N-diisopropylamine; HATU in N,N-dimethyl-formamide T=25°C;
参考文献
Journal of Medicinal Chemistry, , vol. 54, # 21 p. 7579 - 7587
参考文献
US2014/100366 A1, ;
Page/Page column ;
反应条件
1.1: acetic acid / 1,2-dichloro-ethane / 0.25 h 1.2: 24 h / 20 °C 2.1: bis-triphenylphosphine-palladium(II) chloride; sodium carbonate / water; acetonitrile / 0.2 h / 140 °C / Microwave irradiation 3.1: hydrogenchloride / 1,4-dioxane; water / 3 h / 25 °C 4.1: N-ethyl-N,N-diisopropylamine; HATU / N,N-dimethyl-formamide / 25 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 54, # 21 p. 7579 - 7587
反应条件
1: bis-triphenylphosphine-palladium(II) chloride; sodium carbonate / water; acetonitrile / 0.2 h / 140 °C / Microwave irradiation 2: hydrogenchloride / 1,4-dioxane; water / 3 h / 25 °C 3: N-ethyl-N,N-diisopropylamine; HATU / N,N-dimethyl-formamide / 25 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 54, # 21 p. 7579 - 7587
反应条件
1: hydrogenchloride / 1,4-dioxane; water / 3 h / 25 °C 2: N-ethyl-N,N-diisopropylamine; HATU / N,N-dimethyl-formamide / 25 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 54, # 21 p. 7579 - 7587
反应条件
1.1: n-butyllithium / tetrahydrofuran; hexane / 2 h / -78 - -40 °C 1.2: 2 h / -40 °C 1.3: 1 h / Cooling with ice 2.1: acetic acid / 1,2-dichloro-ethane / 0.25 h 2.2: 24 h / 20 °C 3.1: bis-triphenylphosphine-palladium(II) chloride; sodium carbonate / water; acetonitrile / 0.2 h / 140 °C / Microwave irradiation 4.1: hydrogenchloride / 1,4-dioxane; water / 3 h / 25 °C 5.1: N-ethyl-N,N-diisopropylamine; HATU / N,N-dimethyl-formamide / 25 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 54, # 21 p. 7579 - 7587