(2S,3AS,7AS)-1-[2-[乙氧基羰基-(S)-胺基]-(S)-丙酰基八氢吲哚-2-羧酸苄酯]合成路线 (共 12 条)
反应条件
hydrogen; 10 wt platinum on carbon in ethyl acetate T=40°C; P=760.051 Torr;
参考文献
US2007/88168 A1, ;
Page/Page column 2 ;
反应条件
O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate in acetonitrile T=20°C; 0.5 h;
参考文献
WO2007/17087 A1, ;
Page/Page column 13 ;
反应条件
benzotriazol-1-ol; triethylamine; dicyclohexyl-carbodiimide in dichloromethane T=20 - 25°C;
参考文献
EP1679072 A1, ;
Page/Page column 7 ;
反应条件
triethylamine in acetonitrile T=60°C; 4 h; Heating / reflux;
参考文献
US2006/183920 A1, ;
Page/Page column 2 ;
反应条件
1: (2S,3aS,7aS)-2-carboxyperhydroindole benzyl ester benzene sulphonic acid salt With ammonia in dichloromethane; water 0.5 h; 2: (S)-N-[(S)-1-(ethoxycarbonyl)butyl]alanine With benzotriazol-1-ol; dicyclohexyl-carbodiimide in dichloromethane T=10 - 15°C;
参考文献
WO2004/99138 A2, ;
Page 14 ;
反应条件
1: benzyl (S)-(S)-(S)-perhydroindole-2-carboxylate With triethylamine in dichloromethane T=25 - 39°C; 2: N-[1(S)-ethoxycarbonylbutyl]-(S)-alanine-2'-benzothiazolylthio ester in dichloromethane T=-15 - 30°C; 9 - 11 h; Product distribution / selectivity;
参考文献
WO2005/37788 A1, ;
Page/Page column 51 ;
反应条件
1: (2S,3aS,7aS)-2-lt;(benzyloxy)carbonylgt;perhydroindole tosylate; triethylamine in ethyl acetate T=25°C; 2: (S)-N-[(S)-1-(ethoxycarbonyl)butyl]alanine With benzotriazol-1-ol; dicyclohexyl-carbodiimide in ethyl acetate T=15 - 25°C; 3 h; Product distribution / selectivity;
参考文献
WO2005/37788 A1, ;
Page/Page column 42-43 ;
反应条件
triethylamine in dichloromethane T=-15 - 30°C; 0.416667 - 0.5 h; Product distribution / selectivity;
参考文献
WO2005/37788 A1, ;
Page/Page column 47 ;
反应条件
T=20 - 25°C; 5 - 6 h;
参考文献
WO2007/85933 A2, ;
Page/Page column 10-11 ;
反应条件
triethylamine in dichloromethane T=-15 - -10°C; 4 h;
参考文献
Synthetic Communications, , vol. 35, # 2 p. 243 - 248