3,4-二氢异喹啉-2(1h)-甲醛合成路线 （共 30 条）
反应条件
1: 1.) TFAA, 2.) BF3*Et2O / 1.) benzene, RT, 0.5 h, 2.) benzene, RT, 2 h
2: 71 percent / NaBH4, NiCl2*6H2O / methanol; tetrahydrofuran / 0.5 h / Ambient temperature
View Scheme
参考文献
Shinohara, Tatsumi; Toda, Jun; Sano, Takehiro
Chemical and Pharmaceutical Bulletin, 1997 , vol. 45, # 5 p. 813 - 819
反应条件
1: 93 percent / aq. NaIO4 / methanol / 20 h / Ambient temperature
2: 1.) TFAA, 2.) BF3*Et2O / 1.) benzene, RT, 0.5 h, 2.) benzene, RT, 2 h
3: 71 percent / NaBH4, NiCl2*6H2O / methanol; tetrahydrofuran / 0.5 h / Ambient temperature
View Scheme
参考文献
Shinohara, Tatsumi; Toda, Jun; Sano, Takehiro
Chemical and Pharmaceutical Bulletin, 1997 , vol. 45, # 5 p. 813 - 819
反应条件
trifluoroacetic acid
Pictet-Spengler Cyclisation; 4.5 h; Neat (no solvent)Heating / reflux; Product distribution / selectivity;
参考文献
BASF AKTIENGESELLSCHAFT
Patent: WO2006/134143 A1, 2006 ;
Location in patent: Page/Page column 29 ;
反应条件
trifluoroacetic acid
Pictet-Spengler Cyclisation; 4.5 h; Neat (no solvent)Heating / reflux; Product distribution / selectivity;
参考文献
BASF AKTIENGESELLSCHAFT
Patent: WO2006/134143 A1, 2006 ;
Location in patent: Page/Page column 29 ;
反应条件
T=180°C; 4 h; Heating;
参考文献
Venkov, Atanas P.; Ivanov, Ilian I.
Synthetic Communications, 1998 , vol. 28, # 8 p. 1433 - 1438
反应条件
1: 1 h / Heating
2: 57 percent / AcOH/CF3CO2H / 5 h / Heating
View Scheme
参考文献
Lukanov, Ludmil K.; Venkov, Athanas P.; Mollov, Nikola M.
Synthesis, 1987 , # 11 p. 1031 - 1032
参考文献
Suckling, Colin J.; Murphy, John A.; Khalaf, Abedawn I.; Zhou, Sheng-ze; Lizos, Dimitris E.; van Nhien, Albert Nguyen; Yasumatsu, Hiroshi; McVie, Allan; Young, Louise C.; McCraw, Corinna; Waterman, Peter G.; Morris, Brian J.; Pratt, Judith A.; Harvey, Alan L.
Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2649 - 2655
反应条件
in toluene
T=25°C; Ea, ln A; Rate constantThermodynamic data;
参考文献
Maat, L.; Peereboom, M.
Bulletin des Societes Chimiques Belges, 1983 , vol. 92, # 10 p. 877 - 880
参考文献
Judin et al.
Zhurnal Obshchei Khimii, 1957 , vol. 27, p. 3021,3024; engl. Ausg. S. 3051, 3053
反应条件
lithium aluminium tetrahydride in tetrahydrofuran
2 h; Heating;
参考文献
Shinohara, Tatsumi; Toda, Jun; Sano, Takehiro
Chemical and Pharmaceutical Bulletin, 1997 , vol. 45, # 5 p. 813 - 819
