(2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氢-[1,2,4]三唑并[4,3-a]吡嗪-7(8H)-基]-1-(2,4,5-三氟苯基)丁-2-烯-2-胺合成路线 (共 4 条)
反应条件
ammonium acetate in methanol T=40 - 45°C; Large scale reaction;
参考文献
Hansen, Karl B.; Hsiao, Yi; Xu, Feng; Rivera, Nelo; Clausen, Andrew; Kubryk, Michele; Krska, Shane; Rosner, Thorsten; Simmons, Bryon; Balsells, Jaume; Ikemoto, Nori; Sun, Yongkui; Spindler, Felix; Malan, Christophe; Grabowski, Edward J. J.; Armstrong III, Joseph D.
Journal of the American Chemical Society, 2009 , vol. 131, # 25 p. 8798 - 8804
反应条件
sodium tetrahydroborate; acetic acid in toluene
T=5 - 10°C; 3 h; Product distribution / selectivity;
参考文献
MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; ESWARAIAH, Sajja; SATYANARAYANA, Revu; KONDAL REDDY, Bairy; SRINIVAS, Aluru
Patent: WO2010/122578 A2, 2010 ;
Location in patent: Page/Page column 53 ;
反应条件
1: With ammonium chloride; [RhCl(η2:η2-cycloocta-1,5-diene)]2; (R)-(S)-PPF-PtBu2 in methanol
T=20°C; 1 h;
2: With hydrogen in methanol
T=50°C; P=5171.62 Torr; 18 h; Product distribution / selectivity;
参考文献
MERCK and CO., INC.
Patent: WO2006/81151 A1, 2006 ;
Location in patent: Page/Page column 14; 15-16 ;
反应条件
hydrogen; bis(1,5-cyclooctadiene)rhodium(I) trifluoromethanesulfonate; (S)-Cy2-p-Tol-Biphemp in 2,2,2-trifluoroethanol
T=20°C; P=5931.67 Torr; 20 h; Product distribution / selectivity;
参考文献
MERCK and CO., INC.; SOLVIAS AG
Patent: WO2005/97733 A1, 2005 ;
Location in patent: Page/Page column 24 ;