(E)-N-[2-(2,3-二氢-6-甲氧基-1H-茚-1-亚基)乙基]丙酰胺合成路线 (共 8 条)
参考文献
Takeda Chemical Industries, Ltd.
Patent: US6034239 A1, 2000 ;
US 6034239 A
反应条件
1.1: NaH / tetrahydrofuran / 20 °C 1.2: tetrahydrofuran / 20 °C 2.1: H2; ethanolic NH3 / Raney-Co 3.1: Et3N / tetrahydrofuran / 0 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 45, # 19 p. 4222 - 4239
反应条件
1: H2; ethanolic NH3 / Raney-Co 2: Et3N / tetrahydrofuran / 0 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 45, # 19 p. 4222 - 4239
反应条件
hydrogen; Ru(OCOCH3)2((S)-2,2'-bis(diphenylphosphino)-1,1'-binaphthyl) in methanol T=70°C; P=68255.5 Torr; 3 h;
参考文献
Fukatsu, Kohji; Uchikawa, Osamu; Kawada, Mitsuru; Yamano, Toru; Yamashita, Masayuki; Kato, Koki; Hirai, Keisuke; Hinuma, Shuji; Miyamoto, Masaomi; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2002 , vol. 45, # 19 p. 4212 - 4221
反应条件
in methanol; hydrogen
参考文献
Takeda Chemical Industries, Ltd.
Patent: US6034239 A1, 2000 ;
US 6034239 A
反应条件
Ru(OCOCH3)2((S)-2,2'-bis(diphenylphosphino)-1,1'-binaphthyl); hydrogen in methanol T=70°C; P=67505.4 Torr; 1 h;
参考文献
Yamano, Toru; Yamashita, Masayuki; Adachi, Mari; Tanaka, Mitsutaka; Matsumoto, Kiyoharu; Kawada, Mitsuru; Uchikawa, Osamu; Fukatsu, Kohji; Ohkawa, Shigenori
Tetrahedron Asymmetry, 2006 , vol. 17, # 2 p. 184 - 190
反应条件
1.1: 86 percent / NaOAc; Br2 / 0 °C 2.1: 94 percent / BBr3 / CH2Cl2 / 0.67 h / -20 - 20 °C 3.1: NaH / dimethylformamide / 0 °C 3.2: 96 percent / dimethylformamide / 0 °C 4.1: 80 percent / various solvent(s) / 200 - 205 °C View Scheme
参考文献
Uchikawa, Osamu; Fukatsu, Kohji; Tokunoh, Ryosuke; Kawada, Mitsuru; Matsumoto, Kiyoharu; Imai, Yumi; Hinuma, Shuji; Kato, Koki; Nishikawa, Hisao; Hirai, Keisuke; Miyamoto, Masaomi; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2002 , vol. 45, # 19 p. 4222 - 4239
反应条件
1.1: 86 percent / NaOAc; Br2 / 0 °C 2.1: 94 percent / BBr3 / CH2Cl2 / 0.67 h / -20 - 20 °C 3.1: NaH / dimethylformamide / 0 °C 3.2: 96 percent / dimethylformamide / 0 °C 4.1: 80 percent / various solvent(s) / 200 - 205 °C 5.1: O3 / methanol / -78 °C 5.2: 99 percent / NaBH4 / methanol / 1 h / -70 - 20 °C 6.1: 91 percent / Et3N; H2 / 10percent Pd/C/H2O / ethanol / 20 °C 7.1: pyridine / 0.83 h / -10 - -5 °C 7.2: 86 percent / Et3N / ethyl acetate / Heating View Scheme
参考文献
Uchikawa, Osamu; Fukatsu, Kohji; Tokunoh, Ryosuke; Kawada, Mitsuru; Matsumoto, Kiyoharu; Imai, Yumi; Hinuma, Shuji; Kato, Koki; Nishikawa, Hisao; Hirai, Keisuke; Miyamoto, Masaomi; Ohkawa, Shigenori
Journal of Medicinal Chemistry, 2002 , vol. 45, # 19 p. 4222 - 4239