3-氨基-1-[5,6-二氢-3-(三氟甲基)-1,2,4-噻唑并[4,3-a]吡嗪-7(8H)-基]-4-(2,4,5-三氟苯基)-2-丁烯-1-酮合成路线 （共 7 条）
反应条件
ammonium acetate; ammonia in methanol; water
T=55°C; 6 h;
参考文献
DR. REDDY'S LABORATORIES LIMITED; DR. REDDY'S LABORATORIES, INC.
Patent: WO2009/85990 A2, 2009 ;
Location in patent: Page/Page column 28 ;
反应条件
ammonium acetate in methanol; water
T=0 - 45°C; 0.25 - 0.5 h;
参考文献
GLENMARK GENERICS LIMITED
Patent: WO2009/84024 A2, 2009 ;
Location in patent: Page/Page column 23-24 ;
反应条件
1.1: 4-(N,N-dimethlyamino)pyridine / acetonitrile / 25 - 30 °C
1.2: 30 - 50 °C
2.1: ammonium hydroxide; ammonium acetate; acetic acid / water; methanol / 6 h / 60 - 65 °C
View Scheme
参考文献
CADILA HEALTHCARE LIMITED
Patent: US2011/213149 A1, 2011 ;
反应条件
1: With methanesulfonic acid; dimethylsulfide borane complex in tetrahydrofuran; isopropyl alcohol
T=-10 - -5°C; 4 h;
2: With ammonium hydroxide in tetrahydrofuran; water; isopropyl alcohol
Product distribution / selectivity;
参考文献
CADILA HEALTHCARE LIMITED
Patent: US2011/213149 A1, 2011 ;
Location in patent: Page/Page column 15 ;
反应条件
sodium tetrahydroborate; methanesulfonic acid in tetrahydrofuran; isopropyl alcohol
T=-5 - 5°C;
参考文献
CADILA HEALTHCARE LIMITED; KOTHARI, Himanshu, Madhusudan; DAVE, Mayank, Ghanshyambhai; PANDEY, Bipin; SHUKLA, Bhavin, Shriprasad
Patent: WO2010/32264 A2, 2010 ;
Location in patent: Page/Page column 62 ;
反应条件
1: dimethylsulfide borane complex; methanesulfonic acid / isopropyl alcohol; tetrahydrofuran / 4 h / -10 - -5 °C
2: methanol
3: sodium hydrogencarbonate / water; methanol
View Scheme
参考文献
ZENTIVA, K.S.; RICHTER, Jindrich; JIRMAN, Josef
Patent: WO2011/113399 A1, 2011 ;
Location in patent: Page/Page column 6-9 ;
反应条件
[RhCl(η2:η2-cycloocta-1,5-diene)]2; {(S)-1-[(R)-(diphenylphosphino)ferrocenyl]}ethyl-di-tert-butylphosphine; hydrogen; ammonium chloride in methanol
T=50°C; P=5947.36 Torr; 16 h; enantioselective reaction;
参考文献
CADILA HEALTHCARE LIMITED
Patent: US2011/213149 A1, 2011 ;
