3-甲酰吲哚-6-羧酸甲酯合成路线 (共 6 条)
反应条件
tert.-butylhydroperoxide; Cl2Ru*(x)H2O; 2-oxo-3,3-dimethyl-butanoic acid in N-methyl-acetamide T=25°C; 24 h; Inert atmosphere; regioselective reaction;
参考文献
Journal of the American Chemical Society, , vol. 133, # 31 p. 11924 - 11927
反应条件
1: 1.) p-toluenesulfonic acid, p-toluenesulfonyl hydrazide, sulfolane, 2.) NaCNBH3 / 1.) DMF, 100 deg C, 2.) DMF, 100 deg C, 2 h 2: 90 percent / aq. LiOH / methanol / 70 °C View Scheme
参考文献
Hulme, Christopher; Moriarty, Kevin; Miller, Bruce; Mathew, Rose; Ramanjulu, Mercy; Cox, Paul; Souness, John; Page, Ken M.; Uhl, Joanne; Travis, Jeffrey; Huang, Fu-Chih; Labaudiniere, Richard; Djuric, Stevan W.
Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 14 p. 1867 - 1872
反应条件
sulfolane; sodium cyanoborohydride; toluene-4-sulfonic acid; toluene-4-sulfonic acid hydrazide 1.) DMF, 100 deg C, 2.) DMF, 100 deg C, 2 h; Yield given. Multistep reaction;
参考文献
NOVARTIS AG; NOVARTIS PHARMA GMBH
Patent: WO2006/100036 A1, 2006 ;
Location in patent: Page/Page column 159-160 ;
WO 2006/100036 A1
反应条件
sodium cyanoborohydride; toluene-4-sulfonic acid in N-methyl-acetamide; (2S)-N-methyl-1-phenylpropan-2-amine hydrate; water
参考文献
Rhone-Poulenc Rorer Limited
Patent: US6303600 B1, 2001 ;
US 6303600 B1
反应条件
4-(N,N-dimethlyamino)pyridine in acetonitrile
T=20°C;
参考文献
KATHOLIEKE UNIVERSITEIT LEUVEN; BARDIOT, Dorothée; CARLENS, Gunter; DALLMEIER, Kai; KAPTEIN, Suzanne; McNAUGHTON, Michael; MARCHAND, Arnaud; NEYTS, Johan; SMETS, Wim
Patent: WO2013/45516 A1, 2013 ;
Location in patent: Page/Page column 129; 160 ;
反应条件
1: With lithium hydroxide; water in tetrahydrofuran
24 h;
2: With hydrogenchloride; water in tetrahydrofuran
T=0°C;
参考文献
Santillan Jr., Alejandro; McClure, Kelly J.; Allison, Brett D.; Lord, Brian; Boggs, Jamin D.; Morton, Kirsten L.; Everson, Anita M.; Nepomuceno, Diane; Letavic, Michael A.; Lee-Dutra, Alice; Lovenberg, Timothy W.; Carruthers, Nicholas I.; Grice, Cheryl A.
Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 21 p. 6226 - 6230