(E)-2-(3,4-二甲氧基苯基)-3-氟丙-2-烯-1-胺盐酸盐合成路线 (共 6 条)
反应条件
1: 1.) LDA / 1.) THF, -78 deg C, 1h, 2.) THF, overnight
2: 1.) sodium tert-butoxide / 1.) THF, 15 min, 2.) THF, 30 min
3: trifluoroacetic acid / 1 h / Ambient temperature
4: 2M aq. NaOH / tetrahydrofuran / 0.25 h / Ambient temperature
5: 74 percent / 1M Dibal / hexane; CH2Cl2 / 1 h / Ambient temperature
6: 41 percent / triphenylphosphine, diethyl azodiacrboxylate / tetrahydrofuran
7: 1.) hydrazine hydrate, 2.) 18percent aq.HCl / 1.) methanol, reflux, 3 h, 2.) methanol, reflux, 30 min
View Scheme
参考文献
McDonald; Lacoste; Bey; Palfreyman; Zreika
Journal of Medicinal Chemistry, 1985 , vol. 28, # 2 p. 186 - 193
反应条件
1: 74 percent / 1M Dibal / hexane; CH2Cl2 / 1 h / Ambient temperature
2: 41 percent / triphenylphosphine, diethyl azodiacrboxylate / tetrahydrofuran
3: 1.) hydrazine hydrate, 2.) 18percent aq.HCl / 1.) methanol, reflux, 3 h, 2.) methanol, reflux, 30 min
View Scheme
参考文献
McDonald; Lacoste; Bey; Palfreyman; Zreika
Journal of Medicinal Chemistry, 1985 , vol. 28, # 2 p. 186 - 193
反应条件
1: 1.) sodium tert-butoxide / 1.) THF, 15 min, 2.) THF, 30 min
2: trifluoroacetic acid / 1 h / Ambient temperature
3: 2M aq. NaOH / tetrahydrofuran / 0.25 h / Ambient temperature
4: 74 percent / 1M Dibal / hexane; CH2Cl2 / 1 h / Ambient temperature
5: 41 percent / triphenylphosphine, diethyl azodiacrboxylate / tetrahydrofuran
6: 1.) hydrazine hydrate, 2.) 18percent aq.HCl / 1.) methanol, reflux, 3 h, 2.) methanol, reflux, 30 min
View Scheme
参考文献
McDonald; Lacoste; Bey; Palfreyman; Zreika
Journal of Medicinal Chemistry, 1985 , vol. 28, # 2 p. 186 - 193
反应条件
1: trifluoroacetic acid / 1 h / Ambient temperature
2: 2M aq. NaOH / tetrahydrofuran / 0.25 h / Ambient temperature
3: 74 percent / 1M Dibal / hexane; CH2Cl2 / 1 h / Ambient temperature
4: 41 percent / triphenylphosphine, diethyl azodiacrboxylate / tetrahydrofuran
5: 1.) hydrazine hydrate, 2.) 18percent aq.HCl / 1.) methanol, reflux, 3 h, 2.) methanol, reflux, 30 min
View Scheme
参考文献
McDonald; Lacoste; Bey; Palfreyman; Zreika
Journal of Medicinal Chemistry, 1985 , vol. 28, # 2 p. 186 - 193
反应条件
1: 41 percent / triphenylphosphine, diethyl azodiacrboxylate / tetrahydrofuran
2: 1.) hydrazine hydrate, 2.) 18percent aq.HCl / 1.) methanol, reflux, 3 h, 2.) methanol, reflux, 30 min
View Scheme
参考文献
McDonald; Lacoste; Bey; Palfreyman; Zreika
Journal of Medicinal Chemistry, 1985 , vol. 28, # 2 p. 186 - 193
反应条件
hydrogenchloride; hydrazine hydrate
1.) methanol, reflux, 3 h, 2.) methanol, reflux, 30 min; Yield given. Multistep reaction;
参考文献
McDonald; Lacoste; Bey; Palfreyman; Zreika
Journal of Medicinal Chemistry, 1985 , vol. 28, # 2 p. 186 - 193