7-氟-5-甲基-1H-吲哚合成路线 （共 9 条）
反应条件
sodium tetrahydroborate in 1,4-dioxane; water
T=20°C; Reflux;
参考文献
MERCK SHARP andamp; DOHME CORP.; CHUNG, John, Y., L.; ZHANG, Yanfeng; ARTINO, Laura; BAXTER, Jennifer; COTE, Aaron, S.; DESMOND, Donal; SCOTT, Jeremy; VAYNSHTEYN, Yekaterina
Patent: WO2010/80971 A1, 2010 ;
Location in patent: Page/Page column 20 ;
WO 2010/080971 A1
反应条件
1: With N,N-dicyclohexylamine; bis(η3-allyl-μ-chloropalladium(II)); bis[2-(diphenylphosphino)phenyl] ether in n-heptane; toluene
T=70°C; P=1725.17 Torr; 17 h; Inert atmosphere;
2: With tetrabutyl ammonium fluoride in tetrahydrofuran; methanol; n-heptane; toluene
T=80 - 85°C;
参考文献
MERCK SHARP andamp; DOHME CORP.; CHUNG, John, Y., L.; ZHANG, Yanfeng; ARTINO, Laura; BAXTER, Jennifer; COTE, Aaron, S.; DESMOND, Donal; SCOTT, Jeremy; VAYNSHTEYN, Yekaterina
Patent: WO2010/80971 A1, 2010 ;
Location in patent: Page/Page column 18-19 ;
WO 2010/080971 A1
反应条件
1: in tetrahydrofuran
T=-40°C; 1 h;
2: With water; ammonium chloride in tetrahydrofuran
T=20°C; 1 h;
参考文献
Kissei Pharmaceutical Co., Ltd.
Patent: EP1813611 A1, 2007 ;
Location in patent: Page/Page column 16 ;
反应条件
trifluoroacetic acid in tetrahydrofuran; methanol; toluene
T=30 - 85°C; 5 h;
参考文献
Chung, John Y. L.; Steinhuebel, Dietrich; Krska, Shane W.; Hartner, Fred W.; Cai, Chaoxian; Rosen, Jonathan; Mancheno, Danny E.; Pei, Tao; Dimichele, Lisa; Ball, Richard G.; Chen, Cheng-Yi; Tan, Lushi; Alorati, Antony D.; Brewer, Sarah E.; Scott, Jeremy P.
Organic Process Research and Development, 2012 , vol. 16, # 11 p. 1832 - 1845
参考文献
Chung, John Y. L.; Steinhuebel, Dietrich; Krska, Shane W.; Hartner, Fred W.; Cai, Chaoxian; Rosen, Jonathan; Mancheno, Danny E.; Pei, Tao; Dimichele, Lisa; Ball, Richard G.; Chen, Cheng-Yi; Tan, Lushi; Alorati, Antony D.; Brewer, Sarah E.; Scott, Jeremy P.
Organic Process Research and Development, 2012 , vol. 16, # 11 p. 1832 - 1845
反应条件
1.1: calcium carbonate / methanol / 20 - 25 °C
1.2: 6 h / -3 - 2 °C
2.1: N,N-dicyclohexylmethylamine / toluene / 2 h / |Inert atmosphere
2.2: 72 - 75 °C / |Inert atmosphere
3.1: trifluoroacetic acid / methanol; toluene; tetrahydrofuran / 5 h / 30 - 85 °C
View Scheme
参考文献
Chung, John Y. L.; Steinhuebel, Dietrich; Krska, Shane W.; Hartner, Fred W.; Cai, Chaoxian; Rosen, Jonathan; Mancheno, Danny E.; Pei, Tao; Dimichele, Lisa; Ball, Richard G.; Chen, Cheng-Yi; Tan, Lushi; Alorati, Antony D.; Brewer, Sarah E.; Scott, Jeremy P.
Organic Process Research and Development, 2012 , vol. 16, # 11 p. 1832 - 1845
反应条件
1.1: N,N-dicyclohexylmethylamine / toluene / 2 h / |Inert atmosphere
1.2: 72 - 75 °C / |Inert atmosphere
2.1: trifluoroacetic acid / methanol; toluene; tetrahydrofuran / 5 h / 30 - 85 °C
View Scheme
参考文献
Chung, John Y. L.; Steinhuebel, Dietrich; Krska, Shane W.; Hartner, Fred W.; Cai, Chaoxian; Rosen, Jonathan; Mancheno, Danny E.; Pei, Tao; Dimichele, Lisa; Ball, Richard G.; Chen, Cheng-Yi; Tan, Lushi; Alorati, Antony D.; Brewer, Sarah E.; Scott, Jeremy P.
Organic Process Research and Development, 2012 , vol. 16, # 11 p. 1832 - 1845
反应条件
1: bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide; triethylamine
2: copper(l) iodide / N,N-dimethyl-formamide / 100 °C
View Scheme
参考文献
Chung, John Y. L.; Steinhuebel, Dietrich; Krska, Shane W.; Hartner, Fred W.; Cai, Chaoxian; Rosen, Jonathan; Mancheno, Danny E.; Pei, Tao; Dimichele, Lisa; Ball, Richard G.; Chen, Cheng-Yi; Tan, Lushi; Alorati, Antony D.; Brewer, Sarah E.; Scott, Jeremy P.
Organic Process Research and Development, 2012 , vol. 16, # 11 p. 1832 - 1845
反应条件
1: potassium tert-butylate / n-heptane
2: NaAuCl3
View Scheme
参考文献
Chung, John Y. L.; Steinhuebel, Dietrich; Krska, Shane W.; Hartner, Fred W.; Cai, Chaoxian; Rosen, Jonathan; Mancheno, Danny E.; Pei, Tao; Dimichele, Lisa; Ball, Richard G.; Chen, Cheng-Yi; Tan, Lushi; Alorati, Antony D.; Brewer, Sarah E.; Scott, Jeremy P.
Organic Process Research and Development, 2012 , vol. 16, # 11 p. 1832 - 1845
