6-氧代-2-苯基-5-[[(苯基甲氧基)羰基]氨基]-1(6h)-嘧啶乙酸合成路线 (共 13 条)
反应条件
1: 1.83 g / diethyl ether; methanol / 0 °C 2: 95 percent / hydrogen; HCl / Pd-C / ethyl acetate; methanol / 2 h / 20 °C 3: 93 percent / tetrahydrofuran / 120 h / Heating 4: 1.07 g / sodium hydroxide / methanol / 2 h / 20 °C View Scheme
参考文献
Ohmoto, Kazuyuki; Okuma, Motohiro; Yamamoto, Tetsuya; Kijima, Hideomi; Sekioka, Tomohiko; Kitagawa, Kanji; Yamamoto, Shigeki; Tanaka, Kenji; Kawabata, Kazuhito; Sakata, Atsushi; Imawaka, Haruo; Nakai, Hisao; Toda, Masaaki
Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 5 p. 1307 - 1323
反应条件
1: 1.83 g / diethyl ether; methanol / 0 °C 2: 95 percent / hydrogen; HCl / Pd-C / ethyl acetate; methanol / 2 h / 20 °C 3: 93 percent / tetrahydrofuran / 120 h / Heating View Scheme
参考文献
Ohmoto, Kazuyuki; Okuma, Motohiro; Yamamoto, Tetsuya; Kijima, Hideomi; Sekioka, Tomohiko; Kitagawa, Kanji; Yamamoto, Shigeki; Tanaka, Kenji; Kawabata, Kazuhito; Sakata, Atsushi; Imawaka, Haruo; Nakai, Hisao; Toda, Masaaki
Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 5 p. 1307 - 1323
反应条件
1: With sodium chlorite; sodium dihydrogenphosphate in tetrahydrofuran; 2-methyl-but-2-ene; water; tert-butyl alcohol
T=0 - 20°C; 1.16667 h;
2: With hydrogenchloride; sodium hydrogencarbonate in tetrahydrofuran; 2-methyl-but-2-ene; water; tert-butyl alcohol
pH=3;
参考文献
Pharmacia Corporation
Patent: US6653316 B1, 2003 ;
Location in patent: Page/Page column 109-110 ;
US 6653316 B1
反应条件
in water
pH=6 - 8; 3 h;
参考文献
Takahashi, Daisuke; Honda, Yutaka; Izawa, Kunisuke
Heterocycles, 2012 , vol. 85, # 5 p. 1089 - 1103
反应条件
in water; tert-butyl alcohol
参考文献
Imperial Chemical Industries PLC
Patent: US5254558 A1, 1993 ;
反应条件
1: aq. HCl / acetic acid / 2 h / 70 °C
2: NaClO2; NaH2PO4; 2-methyl-2-butene / 2-methyl-propan-2-ol; H2O / 3 h / 0 - 20 °C
View Scheme
参考文献
Ohmoto; Yamamoto; Horiuchi; Kojima; Hachiya; Hashimoto; Kawamura; Nakai; Toda
Synlett, 2001 , # 2 p. 299 - 301
反应条件
1: methanol / 72 h / 5 °C
2: methanol / 1.5 h / 100 °C
3: pyridine, lithium iodide / 2 h / Heating
4: 1.) Et3N, diphenyl phosphorazidate / 1.) 100 deg C, 2 h, 2.) 100 deg C, 12 h
5: 1N aq. HCl / tetrahydrofuran / 8 h / Heating
6: sodium chlorite, sodium dihydrogen phosphate monohydrate / tetrahydrofuran; 2-methyl-propan-2-ol; various solvent(s) / 1 h / Ambient temperature
View Scheme
参考文献
Veale; Bernstein; Bryant; Ceccarelli; Damewood Jr.; Earley; Feeney; Gomes; Kosmider; Steelman; Thomas; Vacek; Williams; Wolanin; Woolson
Journal of Medicinal Chemistry, 1995 , vol. 38, # 1 p. 98 - 108
反应条件
1: HCl / ethanol / 16 h / Ambient temperature
2: methanol / 72 h / 5 °C
3: methanol / 1.5 h / 100 °C
4: pyridine, lithium iodide / 2 h / Heating
5: 1.) Et3N, diphenyl phosphorazidate / 1.) 100 deg C, 2 h, 2.) 100 deg C, 12 h
6: 1N aq. HCl / tetrahydrofuran / 8 h / Heating
7: sodium chlorite, sodium dihydrogen phosphate monohydrate / tetrahydrofuran; 2-methyl-propan-2-ol; various solvent(s) / 1 h / Ambient temperature
View Scheme
参考文献
Veale; Bernstein; Bryant; Ceccarelli; Damewood Jr.; Earley; Feeney; Gomes; Kosmider; Steelman; Thomas; Vacek; Williams; Wolanin; Woolson
Journal of Medicinal Chemistry, 1995 , vol. 38, # 1 p. 98 - 108
反应条件
1: NaHCO3 / tetrahydrofuran; H2O / 0 °C
2: aq. HCl / acetic acid / 2 h / 70 °C
3: NaClO2; NaH2PO4; 2-methyl-2-butene / 2-methyl-propan-2-ol; H2O / 3 h / 0 - 20 °C
View Scheme
参考文献
Ohmoto; Yamamoto; Horiuchi; Kojima; Hachiya; Hashimoto; Kawamura; Nakai; Toda
Synlett, 2001 , # 2 p. 299 - 301
反应条件
1: NaHCO3 / tetrahydrofuran; H2O / 0 °C
2: aq. HCl / acetic acid / 2 h / 70 °C
3: NaClO2; NaH2PO4; 2-methyl-2-butene / 2-methyl-propan-2-ol; H2O / 3 h / 0 - 20 °C
View Scheme
参考文献
Ohmoto; Yamamoto; Horiuchi; Kojima; Hachiya; Hashimoto; Kawamura; Nakai; Toda
Synlett, 2001 , # 2 p. 299 - 301