[3-(2,6-二氯苯基)-5-异丙基异恶唑-4-基]甲醇合成路线 （共 8 条）
反应条件
diisobutylaluminium hydride in tetrahydrofuran T=20°C; Reduction; 16 h;
参考文献
SmithKline Beecham Corporation
Patent: US6639078 B1, 2003 ;
Location in patent: Page/Page column 15 ;
反应条件
1: With lithium aluminium tetrahydride in tetrahydrofuran T=0 - 20°C; 2 h; Inert atmosphere; 2: With methanol in tetrahydrofuran T=0°C; 0.166667 h;
参考文献
Phenex Pharmaceuticals AG
Patent: EP2289883 A1, 2011 ;
Location in patent: Page/Page column 12-13 ;
EP 2289883 A1
反应条件
1.1: 96 percent / OHNH2; NaOH / H2O; ethanol / 24 h / 90 °C 2.1: NCS / dimethylformamide / 1 h / 20 °C 2.2: 3.1 g / NaOMe / tetrahydrofuran; methanol / 16 h / 20 °C 3.1: 93 percent / DIBAL-H / tetrahydrofuran / 16 h / 20 °C View Scheme
参考文献
Phenex Pharmaceuticals AG
Patent: EP2289883 A1, 2011 ;
EP 2289883 A1
反应条件
1.1: NCS / dimethylformamide / 1 h / 20 °C 1.2: 3.1 g / NaOMe / tetrahydrofuran; methanol / 16 h / 20 °C 2.1: 93 percent / DIBAL-H / tetrahydrofuran / 16 h / 20 °C View Scheme
参考文献
PHENEX PHARMACEUTICALS AG; KREMOSER, Claus; ABEL, Ulrich; STEENECK, Christoph; KINZEL, Olaf
Patent: WO2011/20615 A1, 2011 ;
反应条件
1: With sodium methylate in tetrahydrofuran 2: With diisobutylaluminium hydride in tetrahydrofuran T=0 - 20°C;
参考文献
PHENEX PHARMACEUTICALS AG; KREMOSER, Claus; ABEL, Ulrich; STEENECK, Christoph; KINZEL, Olaf
Patent: WO2011/20615 A1, 2011 ;
反应条件
1.1: N-chloro-succinimide / N,N-dimethyl-formamide / 20 °C 2.1: sodium methylate / tetrahydrofuran; methanol / 16 h / 20 °C 3.1: lithium aluminium tetrahydride / tetrahydrofuran / 0 °C / Inert atmosphere 3.2: 0.17 h / 0 °C View Scheme
参考文献
Phenex Pharmaceuticals AG
Patent: EP2289883 A1, 2011 ;
EP 2289883 A1
反应条件
di-isopropyl azodicarboxylate; thiamine diphosphate in dichloromethane T=20°C; Mitsunobu reaction; 4 h;
参考文献
SmithKline Beecham Corporation
Patent: US6639078 B1, 2003 ;
Location in patent: Page/Page column 15 ;
反应条件
1: 63 percent / TPP; DIAD / CH2Cl2 / 4 h / 20 °C
2: 86 percent / NaH / tetrahydrofuran / 5 h / 20 °C
View Scheme
参考文献
Maloney; Parks; Haffner; Fivush; Chandra; Plunket; Creech; Moore; Wilson; Lewis; Jones; Willson
Journal of Medicinal Chemistry, 2000 , vol. 43, # 16 p. 2971 - 2974
