4-[[(1R)-3-(4-吗啉)-1-[(苯基硫代)甲基]丙基]氨基]-3-[(三氟甲基)磺酰基]苯磺酰胺合成路线 （共 8 条）
反应条件
1: With borane-THF in tetrahydrofuran T=20 - 55°C; 26 h; 2: With hydrogenchloride; methanol T=0 - 65°C; 10 h;
参考文献
WO2008/61208 A2, ;
Page/Page column 38-39 ;
WO 2008/061208 A2
反应条件
N-ethyl-N,N-diisopropylamine in dimethyl sulfoxide T=20°C; 16 h;
参考文献
Synthesis, , # 15 art. no. F04408SS, p. 2398 - 2404
反应条件
1.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 1.5 h / 50 °C 2.1: water; lithium hydroxide hydrate / tetrahydrofuran; methanol / 3 h / 18 - 25 °C 2.2: 0 °C 3.1: N-ethyl-N,N-diisopropylamine; HATU / isobutyramide / 1 h / 18 - 25 °C 4.1: borane-THF / tetrahydrofuran / 18 - 25 °C 4.2: 3 h 4.3: pH ~ 10 View Scheme
反应条件
1.1: chlorosulfonic acid / 18 h / 125 °C 1.2: 1.5 h / -65 - 0 °C 2.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 1.5 h / 50 °C 3.1: water; lithium hydroxide hydrate / tetrahydrofuran; methanol / 3 h / 18 - 25 °C 3.2: 0 °C 4.1: N-ethyl-N,N-diisopropylamine; HATU / isobutyramide / 1 h / 18 - 25 °C 5.1: borane-THF / tetrahydrofuran / 18 - 25 °C 5.2: 3 h 5.3: pH ~ 10 View Scheme
反应条件
1.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 1.5 h / 50 °C 2.1: water; lithium hydroxide hydrate / tetrahydrofuran; methanol / 3 h / 18 - 25 °C 2.2: 0 °C 3.1: N-ethyl-N,N-diisopropylamine; HATU / isobutyramide / 1 h / 18 - 25 °C 4.1: borane-THF / tetrahydrofuran / 18 - 25 °C 4.2: 3 h 4.3: pH ~ 10 View Scheme
反应条件
1.1: N-ethyl-N,N-diisopropylamine; HATU / isobutyramide / 1 h / 18 - 25 °C 2.1: borane-THF / tetrahydrofuran / 18 - 25 °C 2.2: 3 h 2.3: pH ~ 10 View Scheme
反应条件
1.1: 1 h / Reflux 2.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 1.5 h / 50 °C 3.1: water; lithium hydroxide hydrate / tetrahydrofuran; methanol / 3 h / 18 - 25 °C 3.2: 0 °C 4.1: N-ethyl-N,N-diisopropylamine; HATU / isobutyramide / 1 h / 18 - 25 °C 5.1: borane-THF / tetrahydrofuran / 18 - 25 °C 5.2: 3 h 5.3: pH ~ 10 View Scheme
反应条件
1.1: water; lithium hydroxide hydrate / tetrahydrofuran; methanol / 3 h / 18 - 25 °C 1.2: 0 °C 2.1: N-ethyl-N,N-diisopropylamine; HATU / isobutyramide / 1 h / 18 - 25 °C 3.1: borane-THF / tetrahydrofuran / 18 - 25 °C 3.2: 3 h 3.3: pH ~ 10 View Scheme
