2-氯-3,4-二甲氧基苯甲醛合成路线 （共 28 条）
反应条件
1: 100 percent / NaBH4 / aq. ethanol / 1 h / 25 °C
2: 97 percent / 12N aq. HCl
3: 96 percent / dimethylsulfoxide / 1.25 h
4: 74 percent / borane / tetrahydrofuran / 1.5 h / Heating
5: K2CO3 / dimethylformamide / 2 h / 110 °C
View Scheme
参考文献
Weinstock; Ladd; Wilson; Brush; Yim; Gallagher Jr.; McCarthy; Silvestri; Sarau; Flaim
Journal of Medicinal Chemistry, 1986 , vol. 29, # 11 p. 2315 - 2325
反应条件
1: 100 percent / NaBH4 / aq. ethanol / 1 h / 25 °C
2: 97 percent / 12N aq. HCl
3: 96 percent / dimethylsulfoxide / 1.25 h
View Scheme
参考文献
McCarthy, James R.; McCowan, Jefferson; Zimmerman, Mark B.; Wenger, Marcia A.; Emmert, Lee W.
Journal of Medicinal Chemistry, 1986 , vol. 29, # 9 p. 1586 - 1590
反应条件
1: 100 percent / NaBH4 / aq. ethanol / 1 h / 25 °C
2: 97 percent / 12N aq. HCl
3: 96 percent / dimethylsulfoxide / 1.25 h
4: 74 percent / borane / tetrahydrofuran / 1.5 h / Heating
5: 37 percent / 2.5 h / Heating
6: TFA, 36 N aq. H2SO4 / 3.5 h / 25 °C
7: BBr3 / CH2Cl2 / 3 h / 25 °C
View Scheme
参考文献
Weinstock; Ladd; Wilson; Brush; Yim; Gallagher Jr.; McCarthy; Silvestri; Sarau; Flaim
Journal of Medicinal Chemistry, 1986 , vol. 29, # 11 p. 2315 - 2325
反应条件
1: With trifluorormethanesulfonic acid; potassium nitrate in acetic acid
T=20°C; 4 h;
2: With sodium hydrogencarbonate in water
参考文献
SANKYO COMPANY, LIMITED; X-CEPTOR THERAPEUTICS, INC.
Patent: WO2003/106435 A1, 2003 ;
Location in patent: Page 330 ;
WO 03/106435 A1
反应条件
sodium tetrahydroborate in ethanol
T=25°C; 1 h;
参考文献
Weinstock; Ladd; Wilson; Brush; Yim; Gallagher Jr.; McCarthy; Silvestri; Sarau; Flaim
Journal of Medicinal Chemistry, 1986 , vol. 29, # 11 p. 2315 - 2325
反应条件
1: 100 percent / NaBH4 / aq. ethanol / 1 h / 25 °C
2: 97 percent / 12N aq. HCl
View Scheme
参考文献
McCarthy, James R.; McCowan, Jefferson; Zimmerman, Mark B.; Wenger, Marcia A.; Emmert, Lee W.
Journal of Medicinal Chemistry, 1986 , vol. 29, # 9 p. 1586 - 1590
反应条件
1: 95 percent / BBr3 / CH2Cl2
2: 1.) KF; / 1.) DMF, room temperature, 2.5 h, 2.) 115 deg C, 1.5 h;
3: 86 percent / NaBH4 / propan-2-ol / 1 h / 70 °C
4: 89 percent / SOCl2 / CH2Cl2 / 1.5 h / Heating
View Scheme
参考文献
Ross; Franz; Wilson; et al.
Journal of Heterocyclic Chemistry, 1986 , vol. 23, # 6 p. 1805 - 1814
反应条件
1: nitric acid / 2 h / 0 - 65 °C
2: potassium permanganate; water / acetone / 1 h / 60 - 70 °C
View Scheme
参考文献
NOVARTIS AG; DECHANTSREITER, Michael A.; GROB, Jonathan E.; MAC SWEENEY, Aengus; MILTZ, Wolfgang; RANDL, Stefan; SEDRANI, Richard; SELLNER, Holger; SIROCKIN, Finton; VALEUR, Eric
Patent: WO2013/192345 A1, 2013 ;
