3-碘-1-(苯基甲基)-1H-吲唑合成路线 （共 10 条）
反应条件
1: 3-iodo-1H-indazole With sodium hydride in tetrahydrofuran T=20°C; 0.75 h; 2: benzyl bromide in tetrahydrofuran T=20°C; Product distribution / selectivity;
参考文献
HIF BIO, INC.; BIZBIOTECH CO., LTD.
Patent: WO2007/65010 A2, 2007 ;
Location in patent: Page/Page column 85 ;
WO 2007/065010 A2
反应条件
N-iodo-succinimide in acetonitrile T=50°C; 55 h;
参考文献
Hari, Yoshiyuki; Shoji, Yoshimichi; Aoyama, Toyohiko
Synthesis, 2004 , # 8 p. 1183 - 1186
反应条件
1: 90 percent / KOH; I2 / dimethylformamide / 2 h / 25 °C 2: 85 percent / t-BuOK / tetrahydrofuran / 8 h View Scheme
参考文献
Collot, Valerie; Dallemagne, Patrick; Bovy, Philippe R.; Rault, Sylvain
Tetrahedron, 1999 , vol. 55, # 22 p. 6917 - 6922
反应条件
1.1: NaH / tetrahydrofuran / 0.17 h / 0 °C 1.2: 90 percent / tetrahydrofuran / 16 h / 20 °C 2.1: 96 percent / N-iodosuccinimide / acetonitrile / 55 h / 50 °C View Scheme
参考文献
Hari, Yoshiyuki; Shoji, Yoshimichi; Aoyama, Toyohiko
Synthesis, 2004 , # 8 p. 1183 - 1186
反应条件
1.1: NaH / tetrahydrofuran / 0.17 h / 0 °C 1.2: 90 percent / tetrahydrofuran / 16 h / 20 °C 2.1: 96 percent / N-iodosuccinimide / acetonitrile / 55 h / 50 °C View Scheme
参考文献
Hari, Yoshiyuki; Shoji, Yoshimichi; Aoyama, Toyohiko
Synthesis, 2004 , # 8 p. 1183 - 1186
反应条件
1: 1-benzyl-3-iodoindazole With isopropylmagnesium chloride in 2-methyl tetrahydrofuran T=-10°C; 2 h; Inert atmosphere; 2: formaldehyd in 2-methyl tetrahydrofuran T=0°C; 2 h; 3: With phosphoric acid in 2-methyl tetrahydrofuran
参考文献
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.; CARACCIOLO TORCHIAROLO, Giuliano; IACOANGELI, Tommaso; FURLOTTI, Guido
Patent: WO2011/15502 A1, 2011 ;
Location in patent: Page/Page column 19; 20 ;
反应条件
1.1: isopropylmagnesium chloride / tetrahydrofuran / 2 h / -10 °C / Inert atmosphere 1.2: 0 °C 2.1: sodium bis(2-methoxyethoxy)aluminium dihydride / toluene / 0.25 h / 20 °C / Inert atmosphere View Scheme
参考文献
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.; CARACCIOLO TORCHIAROLO, Giuliano; IACOANGELI, Tommaso; FURLOTTI, Guido
Patent: WO2011/15501 A1, 2011 ;
Title/Abstract Full Text Show Details
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.; CARACCIOLO TORCHIAROLO, Giuliano; IACOANGELI, Tommaso; FURLOTTI, Guido
Patent: WO2011/15502 A1, 2011 ;
反应条件
1.1: isopropylmagnesium chloride / 2-methyl tetrahydrofuran / 2 h / -10 °C / Inert atmosphere 1.2: 2 h / 0 °C 2.1: hydrogenchloride / toluene; water / 2 h / 90 °C 3.1: sodium hydride / N,N-dimethyl-formamide; toluene / 1.5 h / Inert atmosphere 3.2: 10 h / 90 °C 4.1: sodium hydroxide / 3 h / Reflux View Scheme
参考文献
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.; CARACCIOLO TORCHIAROLO, Giuliano; IACOANGELI, Tommaso; FURLOTTI, Guido
Patent: WO2011/15502 A1, 2011 ;
反应条件
tris(dibenzylideneacetone)dipalladium (0); triphenyl-arsane in N,N-dimethyl-formamide Stille coupling; 16 h;
参考文献
Hering, Kirk W.; Artz, Jennifer D.; Pearson, William H.; Marletta, Michael A.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 3 p. 618 - 621
反应条件
1: 79 percent / sodium hydrogen carbonate / tetrakis(triphenylphosphine)palladium(0) / 1,2-dimethoxy-ethane; H2O / 3 h / Heating 2: 80 percent / phosphorus oxychloride / 0.67 h / 0 - 50 °C 3: 90 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme
参考文献
An, Hongchan; Kim, Nam-Jung; Jung, Jong-Wha; Jang, Hannah; Park, Jong-Wan; Suh, Young-Ger
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6297 - 6300
