4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醛合成路线 （共 37 条）
反应条件
1.1: acetonitrile / 12 h / 84 °C 2.1: hydrogen fluoride / acetonitrile / 6.5 h / 0 - 28 °C 2.2: 0.33 h / pH 8 3.1: diethyl methoxy borane / tetrahydrofuran; methanol / 1.5 h / -85 °C / Inert atmosphere 3.2: 12.5 h / -85 - 30 °C 4.1: water / acetonitrile / 2.75 h / 40 °C 5.1: hydrogenchloride / diethyl ether; water / 0.5 h / pH 5 View Scheme
参考文献
Changzhou Pharmaceutical Factory
Patent: EP2298745 A1, 2011 ;
反应条件
1: 71.3 percent / acetonitrile / 14 h / Heating 2: 13 g / HF / acetonitrile / 1.5 h / Ambient temperature 3: 1.) Et2BOMe, 2.) NaBH4 / 1.) THF, MeOH, -78 deg C, 30 min, 2.) THF, MeOH, 3 h View Scheme
参考文献
JUBILANT LIFE SCIENCES LTD.; SINGH, Khushwant; SINGH, Anand, Kumar; SRIVASTAVA, Rahul; KUMAR, Pramod; VIR, Dharam; AGARWAL, Ashutosh
Patent: WO2012/63115 A2, 2012 ;
反应条件
1: in acetonitrile 20 h; Reflux; 2: With hydrogen fluoride in acetonitrile T=20°C; 3 h; Cooling with ice; 3: With sodium hydrogencarbonate in dichloromethane; water; acetonitrile
参考文献
MATRIX LABORATORIES LTD.; SETHI, Madhuresh, Kumar; MAHAJAN, Sanjay; RAWAT, Vijendra, Singh; MARA, Bhairaiah; VEERA, Upendra, Nath; DATTA, Debashish
Patent: WO2011/141934 A1, 2011 ;
Location in patent: Page/Page column 17; 18-19 ;
反应条件
1: 71.3 percent / acetonitrile / 14 h / Heating 2: 13 g / HF / acetonitrile / 1.5 h / Ambient temperature View Scheme
参考文献
JUBILANT LIFE SCIENCES LTD.; SINGH, Khushwant; SINGH, Anand, Kumar; SRIVASTAVA, Rahul; KUMAR, Pramod; VIR, Dharam; AGARWAL, Ashutosh
Patent: WO2012/63115 A2, 2012 ;
反应条件
methanol; sodium tetrahydroborate in tetrahydrofuran T=5 - 10°C;
参考文献
BIOCON LIMITED; ANEGONDI, Sreenivasa, Prasad; RAJMAHENDRA, Shanmughasamy; JOSEPH, Jibin; SRINIVAS, Pullela, Venkata
Patent: WO2010/23678 A1, 2010 ;
Location in patent: Page/Page column 15 ;
反应条件
in toluene Wittig condensation; 30 h; Heating / reflux;
参考文献
ORCHID CHEMICALS and PHARMACEUTICALS LIMITED
Patent: WO2008/93205 A2, 2008 ;
Location in patent: Page/Page column 7-8 ;
反应条件
in acetonitrile
15 h; Reflux; Product distribution / selectivity;
参考文献
IND-SWIFT LABORATORIES LIMITED; BHIRUD Shekhar Bhaskar; JAIN Anshul Kumar; SAINI Vinay Kumar; SHARMA Alok
Patent: WO2012/176218 A1, 2012 ;
Location in patent: Page/Page column 18 ;
