2,6-二氨基-4,5,6,7-四氢苯并噻唑合成路线 (共 15 条)
反应条件
triethylamine; hydrazine in isopropyl alcohol 2 - 3 h; Heating / reflux;
参考文献
WO2006/3677 A1, ;
Page/Page column 10; 18 ;
反应条件
1: With hydrogen bromide in water Heating / reflux; 2: With sodium hydroxide in water T=10°C;
参考文献
WO2004/41797 A1, ;
Page 2; 5-6 ;
反应条件
1: trans-4-amino-cyclohexanol With acetic anhydride in N,N-dimethyl-formamide T=10 - 15°C; 2: With Jone's reagent in acetone T=10 - 15°C; 3 h; 3: thiourea With sodium hydroxide; water; hydrogen bromide; bromine Product distribution / selectivity; more than 3 stages;
参考文献
WO2008/104847 A2, ;
Page/Page column 11-12 ;
反应条件
in acetic acid T=80°C; 3 h; Product distribution / selectivity;
参考文献
WO2008/104847 A2, ;
Page/Page column 11 ;
反应条件
1.1: bromine; acetic acid / 0.75 h / 25 - 35 °C 1.2: 3 h / Reflux 2.1: water; sulfuric acid / 10 h / Reflux 2.2: 1.5 h / 0 - 30 °C View Scheme
反应条件
water; hydrogen bromide 15 h; Reflux;
参考文献
Investigational New Drugs, , vol. 28, # 4 p. 454 - 465
反应条件
2: 84 percent / triethylamine / tetrahydrofuran / 2 h / -5 °C View Scheme
参考文献
Schneider, Claus S.; Mierau, Joachim
Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 494 - 498
反应条件
optical resolution with chiral tartaric acid;
参考文献
AMR TECHNOLOGY, INC.
Patent: WO2006/12276 A1, 2006 ;
Location in patent: Page/Page column 16-17 ;
参考文献
Schneider, Claus S.; Mierau, Joachim
Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 494 - 498
反应条件
1.1: water / 70 °C / Reflux; Resolution of racemate 2.1: hydrogenchloride / water / carbon treatment 2.2: 1.5 h / 25 - 30 °C 3.1: triethylamine / methanol / 1.5 h / 10 - 20 °C 4.1: sodium tetrahydroborate; boron trifluoride diethyl etherate / tetrahydrofuran / 4 h / 0 - 50 °C 4.2: 0.17 h / 10 °C 5.1: hydrogenchloride / water; methanol / 0.75 h / 25 - 30 °C View Scheme
参考文献
MSN LABORATORIES LIMITED; SATYANARAYANA REDDY, Manne; ESWARAIAH, Sajja; SAHADEVA REDDY, Maramreddy
Patent: WO2011/21214 A2, 2011 ;