7-氟-8-(4-甲基-1-哌嗪基)-5-氧代-5H-噻唑并[3,2-a]喹啉-4-羧酸合成路线 (共 9 条)
参考文献
Nippon Shinyaku Co., Ltd.
Patent: US4659734 A1, 1987 ;
反应条件
in pyridine
75 h; Heating;
参考文献
Segawa; Kitano; Kazuno; Tsuda; Shirahase; Ozaki; Matsuda; Kise
Journal of Heterocyclic Chemistry, 1992 , vol. 29, # 5 p. 1117 - 1123
反应条件
1: 0 °C
2: triethylamine, ethyl chloroformate / CHCl3 / 3.5 h / Ambient temperature
3: 1.) sodium hydride / 1.) THF, RT, 1 h, 2.) THF, RT, 1 h
4: dimethylformamide / 2 h / Ambient temperature
5: diphenyl ether / 0.2 h / 250 °C
6: 84 percent / trifluoromethanesulfonic acid, trifluoroacetic acid, anisole / 2 h / Ambient temperature
7: 1.) potassium bicarbonate / 1.) DMF, 80 deg, 12 h, 2.) conc. sulfuric acid, 90 deg, 20 min.
8: 73 percent / sodium hydroxide, water / ethanol / 2 h / Heating
9: 52 percent / pyridine / 75 h / Heating
View Scheme
参考文献
Segawa; Kitano; Kazuno; Tsuda; Shirahase; Ozaki; Matsuda; Kise
Journal of Heterocyclic Chemistry, 1992 , vol. 29, # 5 p. 1117 - 1123
反应条件
1: 1.) sodium hydride / 1.) THF, RT, 1 h, 2.) THF, RT, 1 h
2: dimethylformamide / 2 h / Ambient temperature
3: diphenyl ether / 0.2 h / 250 °C
4: 84 percent / trifluoromethanesulfonic acid, trifluoroacetic acid, anisole / 2 h / Ambient temperature
5: 1.) potassium bicarbonate / 1.) DMF, 80 deg, 12 h, 2.) conc. sulfuric acid, 90 deg, 20 min.
6: 73 percent / sodium hydroxide, water / ethanol / 2 h / Heating
7: 52 percent / pyridine / 75 h / Heating
View Scheme
参考文献
Segawa; Kitano; Kazuno; Tsuda; Shirahase; Ozaki; Matsuda; Kise
Journal of Heterocyclic Chemistry, 1992 , vol. 29, # 5 p. 1117 - 1123
反应条件
1: 1.) potassium bicarbonate / 1.) DMF, 80 deg, 12 h, 2.) conc. sulfuric acid, 90 deg, 20 min.
2: 73 percent / sodium hydroxide, water / ethanol / 2 h / Heating
3: 52 percent / pyridine / 75 h / Heating
View Scheme
参考文献
Segawa; Kitano; Kazuno; Tsuda; Shirahase; Ozaki; Matsuda; Kise
Journal of Heterocyclic Chemistry, 1992 , vol. 29, # 5 p. 1117 - 1123
反应条件
1: 73 percent / sodium hydroxide, water / ethanol / 2 h / Heating
2: 52 percent / pyridine / 75 h / Heating
View Scheme
参考文献
Segawa; Kitano; Kazuno; Tsuda; Shirahase; Ozaki; Matsuda; Kise
Journal of Heterocyclic Chemistry, 1992 , vol. 29, # 5 p. 1117 - 1123
反应条件
1: 84 percent / trifluoromethanesulfonic acid, trifluoroacetic acid, anisole / 2 h / Ambient temperature
2: 1.) potassium bicarbonate / 1.) DMF, 80 deg, 12 h, 2.) conc. sulfuric acid, 90 deg, 20 min.
3: 73 percent / sodium hydroxide, water / ethanol / 2 h / Heating
4: 52 percent / pyridine / 75 h / Heating
View Scheme
参考文献
Segawa; Kitano; Kazuno; Tsuda; Shirahase; Ozaki; Matsuda; Kise
Journal of Heterocyclic Chemistry, 1992 , vol. 29, # 5 p. 1117 - 1123
反应条件
1: diphenyl ether / 0.2 h / 250 °C
2: 84 percent / trifluoromethanesulfonic acid, trifluoroacetic acid, anisole / 2 h / Ambient temperature
3: 1.) potassium bicarbonate / 1.) DMF, 80 deg, 12 h, 2.) conc. sulfuric acid, 90 deg, 20 min.
4: 73 percent / sodium hydroxide, water / ethanol / 2 h / Heating
5: 52 percent / pyridine / 75 h / Heating
View Scheme
参考文献
Segawa; Kitano; Kazuno; Tsuda; Shirahase; Ozaki; Matsuda; Kise
Journal of Heterocyclic Chemistry, 1992 , vol. 29, # 5 p. 1117 - 1123
反应条件
1: dimethylformamide / 2 h / Ambient temperature
2: diphenyl ether / 0.2 h / 250 °C
3: 84 percent / trifluoromethanesulfonic acid, trifluoroacetic acid, anisole / 2 h / Ambient temperature
4: 1.) potassium bicarbonate / 1.) DMF, 80 deg, 12 h, 2.) conc. sulfuric acid, 90 deg, 20 min.
5: 73 percent / sodium hydroxide, water / ethanol / 2 h / Heating
6: 52 percent / pyridine / 75 h / Heating
View Scheme
参考文献
Segawa; Kitano; Kazuno; Tsuda; Shirahase; Ozaki; Matsuda; Kise
Journal of Heterocyclic Chemistry, 1992 , vol. 29, # 5 p. 1117 - 1123