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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
阿鲁司特
合成路线
(共 19 条)
120329-95-5
→
反应条件
96566-25-5
阿鲁司特
反应条件
lithium hydroxide in tetrahydrofuran; water 6 h; Ambient temperature;
参考文献
Cohen, Noal; Weber, Giuseppe; Banner, Bruce L.; Lopresti, Rocco J.; Schaer, Beatrice; et al.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1842 - 1860
122443-78-1
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 81.6 percent / K2CO3 / 18-crown-6 / acetonitrile / 22 h / Heating 2: 96.8 percent / K2CO3 / acetone; dimethylformamide / 5.5 h / Heating 3: 72 percent / LiOH*H2O / tetrahydrofuran; H2O / 6 h / Ambient temperature View Scheme
参考文献
Cohen, Noal; Weber, Giuseppe; Banner, Bruce L.; Lopresti, Rocco J.; Schaer, Beatrice; et al.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1842 - 1860
23866-72-0
7-羟基-4-氧代-4H-苯并吡喃-2-羧酸乙酯
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 73.4 percent / H2 / 10percent Pd/C / acetic acid / 41 h / Ambient temperature 2: 79 percent / pyridine / 24 h / Ambient temperature 3: 1.) BF3*Et2O, AcOH, Ac2O, 2.) p-TsOH*H2O / 1.) reflux, 18.5 h, 2.) reflux, 20 h 4: 82.2 percent / K2CO3 / acetone; dimethylformamide / 27 h / Heating 5: K2CO3 / acetone; dimethylformamide / 5.5 h / Heating 6: LiOH*H2O / tetrahydrofuran; H2O / 6 h / Ambient temperature View Scheme
参考文献
Cohen, Noal; Weber, Giuseppe; Banner, Bruce L.; Lopresti, Rocco J.; Schaer, Beatrice; et al.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1842 - 1860
111-24-0
二溴戊烷
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 81.6 percent / K2CO3 / 18-crown-6 / acetonitrile / 22 h / Heating 2: 96.8 percent / K2CO3 / acetone; dimethylformamide / 5.5 h / Heating 3: 72 percent / LiOH*H2O / tetrahydrofuran; H2O / 6 h / Ambient temperature View Scheme
参考文献
Cohen, Noal; Weber, Giuseppe; Banner, Bruce L.; Lopresti, Rocco J.; Schaer, Beatrice; et al.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1842 - 1860
89-84-9
2,4-二羟基苯乙酮
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 86 percent / NaOEt / ethanol / 3 h / 50 °C 2: 85 percent / H2 / 10 percent Pd/C / acetic acid; tetrahydrofuran / 45 °C / 3361.5 Torr 3: BF3*OEt2 / acetic acid / 18 h / Heating 4: p-toluenesulfonic acid / 18 h / Heating 5: 97 percent / K2CO3 / dimethylsulfoxide / 18 h / Ambient temperature 6: 94 percent / tetrabutylammonium hydroxide / methanol / 3 h / Ambient temperature 7: Et3N / 2 h / 6 °C 8: 81 percent / K2CO3, tris(3,6-dioxa-heptyl)amine / toluene / 6 h / Heating 9: 99 percent / aq. NaOH / methanol / 1.25 h / Heating 10: 2 N HCl View Scheme
参考文献
Manchand; Micheli; Saposnik
Tetrahedron, 1992 , vol. 48, # 43 p. 9391 - 9398
40786-69-4
2,4-二羟基-3-丙基苯乙酮
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 96.8 percent / K2CO3 / acetone; dimethylformamide / 5.5 h / Heating 2: 72 percent / LiOH*H2O / tetrahydrofuran; H2O / 6 h / Ambient temperature View Scheme
参考文献
Cohen, Noal; Weber, Giuseppe; Banner, Bruce L.; Lopresti, Rocco J.; Schaer, Beatrice; et al.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1842 - 1860
96566-14-2
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 79 percent / pyridine / 24 h / Ambient temperature 2: 1.) BF3*Et2O, AcOH, Ac2O, 2.) p-TsOH*H2O / 1.) reflux, 18.5 h, 2.) reflux, 20 h 3: 82.2 percent / K2CO3 / acetone; dimethylformamide / 27 h / Heating 4: K2CO3 / acetone; dimethylformamide / 5.5 h / Heating 5: LiOH*H2O / tetrahydrofuran; H2O / 6 h / Ambient temperature View Scheme
参考文献
Cohen, Noal; Weber, Giuseppe; Banner, Bruce L.; Lopresti, Rocco J.; Schaer, Beatrice; et al.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1842 - 1860
96566-17-5
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 82.2 percent / K2CO3 / acetone; dimethylformamide / 27 h / Heating 2: K2CO3 / acetone; dimethylformamide / 5.5 h / Heating 3: LiOH*H2O / tetrahydrofuran; H2O / 6 h / Ambient temperature View Scheme
参考文献
Cohen, Noal; Weber, Giuseppe; Banner, Bruce L.; Lopresti, Rocco J.; Schaer, Beatrice; et al.
Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1842 - 1860
38987-00-7
1-(3-烯丙基-2,4-二羟基苯基)乙酮
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 96 percent / H2 / 5 percent Pt/C / toluene; tetrahydrofuran / 1551.4 Torr / Ambient temperature 2: 81 percent / K2CO3, tris(3,6-dioxa-heptyl)amine / toluene / 6 h / Heating 3: 99 percent / aq. NaOH / methanol / 1.25 h / Heating 4: 2 N HCl View Scheme
参考文献
Manchand; Micheli; Saposnik
Tetrahedron, 1992 , vol. 48, # 43 p. 9391 - 9398
40815-74-5
→
反应条件
96566-25-5
阿鲁司特
反应条件
1: 80 percent / xylene / 18 h / 215 °C 2: 96 percent / H2 / 5 percent Pt/C / toluene; tetrahydrofuran / 1551.4 Torr / Ambient temperature 3: 81 percent / K2CO3, tris(3,6-dioxa-heptyl)amine / toluene / 6 h / Heating 4: 99 percent / aq. NaOH / methanol / 1.25 h / Heating 5: 2 N HCl View Scheme
参考文献
Manchand; Micheli; Saposnik
Tetrahedron, 1992 , vol. 48, # 43 p. 9391 - 9398
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