(5R-cis)-甲苯-4-磺酸 5-(2,4-二氟苯基)-5-(1H-1,2,4-三氮唑-1-基)甲基四氢呋喃-3-基甲基酯合成路线 （共 20 条）
反应条件
1: C14H15F2N3O2*(x)ClH With triethylamine in dichloromethane T=12 - 22°C; 1 h; 2: p-toluenesulfonyl chloride With 4-(N,N-dimethlyamino)pyridine in dichloromethane T=12 - 25°C; 4 h;
参考文献
SANDOZ AG; OBERHUBER, Michael; SALCHENEGGER, Joerg; DE SOUZA, Dominic; ALBERT, Martin; WILHELM, Thorsten; LANGNER, Martin; STURM, Hubert; SPITZENSTAeTTER, Hans-Peter
Patent: WO2011/144653 A1, 2011 ;
Location in patent: Page/Page column 63-64 ;
反应条件
4-(N,N-dimethlyamino)pyridine in tetrahydrofuran 18 h;
参考文献
Lovey, Raymond G.; Saksena, Anil K.; Girijavallabhan, Viyyoor M.
Tetrahedron Letters, 1994 , vol. 35, # 33 p. 6047 - 6050
反应条件
1: tetrahydrofuran / -78 °C 2: 1.) TiCl4; 2.) Et3N / 1.) CH2Cl2, 0 deg C 3: 85 percent / LAH / tetrahydrofuran / 0 °C 4: 96 percent / I2 / acetonitrile; pyridine / 0 - 5 °C 5: 81 percent / DMPU / dimethylformamide / 24 h / 100 °C 6: 100 percent / H2 / 10percent Pd/C 7: 82 percent / pyridine View Scheme
参考文献
Tetrahedron Letters, , vol. 37, # 32 p. 5657 - 5660
反应条件
1: 96 percent / I2 / acetonitrile; pyridine / 0 - 5 °C 2: 81 percent / DMPU / dimethylformamide / 24 h / 100 °C 3: 100 percent / H2 / 10percent Pd/C 4: 82 percent / pyridine View Scheme
参考文献
Tetrahedron Letters, , vol. 37, # 32 p. 5657 - 5660
反应条件
1: 1.) TiCl4; 2.) Et3N / 1.) CH2Cl2, 0 deg C 2: 85 percent / LAH / tetrahydrofuran / 0 °C 3: 96 percent / I2 / acetonitrile; pyridine / 0 - 5 °C 4: 81 percent / DMPU / dimethylformamide / 24 h / 100 °C 5: 100 percent / H2 / 10percent Pd/C 6: 82 percent / pyridine View Scheme
参考文献
Tetrahedron Letters, , vol. 37, # 32 p. 5657 - 5660
反应条件
1: 85 percent / LAH / tetrahydrofuran / 0 °C 2: 96 percent / I2 / acetonitrile; pyridine / 0 - 5 °C 3: 81 percent / DMPU / dimethylformamide / 24 h / 100 °C 4: 100 percent / H2 / 10percent Pd/C 5: 82 percent / pyridine View Scheme
参考文献
Tetrahedron Letters, , vol. 37, # 32 p. 5657 - 5660
反应条件
1: 78 percent / porcine pancreatic lipase / 48 h / Ambient temperature 2: 98 percent / p-TsOH / CH2Cl2 3: 96 percent / KOH / tetrahydrofuran; H2O / 18 h 4: 96 percent / DMAP / tetrahydrofuran / 18 h 5: 95 percent / NaH / tetrahydrofuran / 1 h 6: 94 percent / p-TsOH / methanol / 24 h 7: 93 percent / DMAP / tetrahydrofuran / 18 h View Scheme
参考文献
Tetrahedron Letters, , vol. 35, # 33 p. 6047 - 6050
反应条件
1: 75 percent / DMPU / dimethylformamide / 24 h / 100 °C 2: 82 percent / pyridine View Scheme
参考文献
Tetrahedron Letters, , vol. 37, # 32 p. 5657 - 5660
反应条件
1: 100 percent / H2 / 10percent Pd/C 2: 82 percent / pyridine View Scheme
参考文献
Tetrahedron Letters, , vol. 37, # 32 p. 5657 - 5660
反应条件
1: 90 percent / LiBH4 / tetrahydrofuran / 1.) -78 deg C up to RT; 2.) RT, 2 h 2: 75 percent / DMPU / dimethylformamide / 24 h / 100 °C 3: 82 percent / pyridine View Scheme
参考文献
Tetrahedron Letters, , vol. 37, # 32 p. 5657 - 5660
