4-氯-2-碘噻吩并[2,3-b]吡啶-5-甲腈合成路线 （共 5 条）
反应条件
1: With lithium diisopropyl amide in tetrahydrofuran; n-heptane; ethylbenzene
T=-78°C; 0.583333 h;
2: With iodine in tetrahydrofuran; n-heptane; ethylbenzene
T=-78°C; 4 h;
参考文献
Boschelli, Diane H.; Wu, Biqi; Sosa, Ana Carolina Barrios; Durutlic, Haris; Ye, Fei; Raifeld, Yuri; Golas, Jennifer M.; Boschelli, Frank
Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6666 - 6668
反应条件
trichlorophosphate in N,N-dimethyl-formamide
T=70°C;
参考文献
Boschelli, Diane Harris; Tumey, Lawrence Nathan; Wu, Biqi
Patent: US2008/76926 A1, 2008 ;
Location in patent: Page/Page column 16 ;
US 20080076926 A1
反应条件
1.1: 480 mg / aq. NaOH / ethanol / 1.5 h / Heating
2.1: thionyl chloride / 2 h / Heating
3.1: 175 mg / aq. ammonia / acetone / 2 h / 0 °C
4.1: 84 mg / cyanuric chloride / dimethylformamide / 0.5 h / 20 °C
5.1: LDA / heptane; tetrahydrofuran; ethylbenzene / 0.58 h / -78 °C
5.2: 1.0 g / iodine / tetrahydrofuran; heptane; ethylbenzene / 4 h / -78 °C
View Scheme
参考文献
Boschelli, Diane H.; Wu, Biqi; Sosa, Ana Carolina Barrios; Durutlic, Haris; Ye, Fei; Raifeld, Yuri; Golas, Jennifer M.; Boschelli, Frank
Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6666 - 6668
反应条件
1.1: 84 mg / cyanuric chloride / dimethylformamide / 0.5 h / 20 °C
2.1: LDA / heptane; tetrahydrofuran; ethylbenzene / 0.58 h / -78 °C
2.2: 1.0 g / iodine / tetrahydrofuran; heptane; ethylbenzene / 4 h / -78 °C
View Scheme
参考文献
Boschelli, Diane H.; Wu, Biqi; Sosa, Ana Carolina Barrios; Durutlic, Haris; Ye, Fei; Raifeld, Yuri; Golas, Jennifer M.; Boschelli, Frank
Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6666 - 6668
反应条件
1.1: thionyl chloride / 2 h / Heating
2.1: 175 mg / aq. ammonia / acetone / 2 h / 0 °C
3.1: 84 mg / cyanuric chloride / dimethylformamide / 0.5 h / 20 °C
4.1: LDA / heptane; tetrahydrofuran; ethylbenzene / 0.58 h / -78 °C
4.2: 1.0 g / iodine / tetrahydrofuran; heptane; ethylbenzene / 4 h / -78 °C
View Scheme
参考文献
Boschelli, Diane H.; Wu, Biqi; Sosa, Ana Carolina Barrios; Durutlic, Haris; Ye, Fei; Raifeld, Yuri; Golas, Jennifer M.; Boschelli, Frank
Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6666 - 6668
