2-(4-氨基苯基)-3-{[苄基(甲基)氨基]甲基}-7-(2,6-二氟苄基)-5-异丁酰基噻吩并[2,3-b]吡啶-4(7H)-酮合成路线 （共 10 条）
反应条件
sodium hydroxide in methanol
T=60°C; 1 h;
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1.1: 60 percent / polyphosphate ester / 120 °C
2.1: 90 percent / K2CO3; KI / dimethylformamide / 20 - 50 °C
3.1: 71 percent / NaNO3; H2SO4 / 0 °C
4.1: N-bromosuccinimide; 2,2'-azobis(isobutyronitrile) / CCl4 / Heating
5.1: N,N-diisopropylethylamine / dimethylformamide / 20 °C
6.1: 96 percent / aq. HCl; Fe / ethanol / 0 °C
7.1: 98 percent / Et3N / CH2Cl2 / 1 h / 20 °C
8.1: Me3Al; N,N-diisopropylethylamine / CH2Cl2; hexane / 0 °C
8.2: 94 percent / CH2Cl2; hexane / 0 °C
9.1: 75 percent / dioxane / 0 °C
10.1: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1.1: KOH / ethanol; dioxane / 70 °C
2.1: 60 percent / polyphosphate ester / 120 °C
3.1: 90 percent / K2CO3; KI / dimethylformamide / 20 - 50 °C
4.1: 71 percent / NaNO3; H2SO4 / 0 °C
5.1: N-bromosuccinimide; 2,2'-azobis(isobutyronitrile) / CCl4 / Heating
6.1: N,N-diisopropylethylamine / dimethylformamide / 20 °C
7.1: 96 percent / aq. HCl; Fe / ethanol / 0 °C
8.1: 98 percent / Et3N / CH2Cl2 / 1 h / 20 °C
9.1: Me3Al; N,N-diisopropylethylamine / CH2Cl2; hexane / 0 °C
9.2: 94 percent / CH2Cl2; hexane / 0 °C
10.1: 75 percent / dioxane / 0 °C
11.1: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1: 75 percent / dioxane / 0 °C
2: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1.1: Me3Al; N,N-diisopropylethylamine / CH2Cl2; hexane / 0 °C
1.2: 94 percent / CH2Cl2; hexane / 0 °C
2.1: 75 percent / dioxane / 0 °C
3.1: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1.1: 90 percent / K2CO3; KI / dimethylformamide / 20 - 50 °C
2.1: 71 percent / NaNO3; H2SO4 / 0 °C
3.1: N-bromosuccinimide; 2,2'-azobis(isobutyronitrile) / CCl4 / Heating
4.1: N,N-diisopropylethylamine / dimethylformamide / 20 °C
5.1: 96 percent / aq. HCl; Fe / ethanol / 0 °C
6.1: 98 percent / Et3N / CH2Cl2 / 1 h / 20 °C
7.1: Me3Al; N,N-diisopropylethylamine / CH2Cl2; hexane / 0 °C
7.2: 94 percent / CH2Cl2; hexane / 0 °C
8.1: 75 percent / dioxane / 0 °C
9.1: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1.1: N-bromosuccinimide; 2,2'-azobis(isobutyronitrile) / CCl4 / Heating
2.1: N,N-diisopropylethylamine / dimethylformamide / 20 °C
3.1: 96 percent / aq. HCl; Fe / ethanol / 0 °C
4.1: 98 percent / Et3N / CH2Cl2 / 1 h / 20 °C
5.1: Me3Al; N,N-diisopropylethylamine / CH2Cl2; hexane / 0 °C
5.2: 94 percent / CH2Cl2; hexane / 0 °C
6.1: 75 percent / dioxane / 0 °C
7.1: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1.1: N,N-diisopropylethylamine / dimethylformamide / 20 °C
2.1: 96 percent / aq. HCl; Fe / ethanol / 0 °C
3.1: 98 percent / Et3N / CH2Cl2 / 1 h / 20 °C
4.1: Me3Al; N,N-diisopropylethylamine / CH2Cl2; hexane / 0 °C
4.2: 94 percent / CH2Cl2; hexane / 0 °C
5.1: 75 percent / dioxane / 0 °C
6.1: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1.1: 98 percent / Et3N / CH2Cl2 / 1 h / 20 °C
2.1: Me3Al; N,N-diisopropylethylamine / CH2Cl2; hexane / 0 °C
2.2: 94 percent / CH2Cl2; hexane / 0 °C
3.1: 75 percent / dioxane / 0 °C
4.1: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
反应条件
1.1: 96 percent / aq. HCl; Fe / ethanol / 0 °C
2.1: 98 percent / Et3N / CH2Cl2 / 1 h / 20 °C
3.1: Me3Al; N,N-diisopropylethylamine / CH2Cl2; hexane / 0 °C
3.2: 94 percent / CH2Cl2; hexane / 0 °C
4.1: 75 percent / dioxane / 0 °C
5.1: 79 percent / aq. NaOH / methanol / 1 h / 60 °C
View Scheme
参考文献
Imada, Takashi; Cho, Nobuo; Imaeda, Toshihiro; Hayase, Yoji; Sasaki, Satoshi; Kasai, Shizuo; Harada, Masataka; Matsumoto, Hirokazu; Endo, Satoshi; Suzuki, Nobuhiro; Furuya, Shuichi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3809 - 3825
