(S)-2,6-二氨基-4,5,6,7-四氢苯并噻唑合成路线 (共 13 条)
反应条件
1: With hydrogenchloride in water Acidic aqueous solution; 2: With sodium hydroxide T=50°C; pH=<= 7; Alkaline aqueous solution;
参考文献
WO2008/86047 A1, ;
Page/Page column 142-144 ;
WO 2008/086047 A1
反应条件
hydrogenchloride; potassium hydroxide in water T=0 - 5°C; 1 - 2 h;
参考文献
ALEMBIC LIMITED
Patent: WO2006/3677 A1, 2006 ;
Location in patent: Page/Page column 10; 18 ;
参考文献
Journal of Medicinal Chemistry, , vol. 30, # 3 p. 494 - 498
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 3.1: water / 70 °C / Reflux; Resolution of racemate 4.1: hydrogenchloride / water / carbon treatment 4.2: 1.5 h / 25 - 30 °C View Scheme
反应条件
1.1: water; sulfuric acid / 10 h / Reflux 1.2: 1.5 h / 0 - 30 °C 2.1: water / 70 °C / Reflux; Resolution of racemate 3.1: hydrogenchloride / water / carbon treatment 3.2: 1.5 h / 25 - 30 °C View Scheme
反应条件
1: water; hydrogen bromide / 15 h / Reflux 2: L-(+)-tartaric acid / 75 °C View Scheme
参考文献
Investigational New Drugs, , vol. 28, # 4 p. 454 - 465
反应条件
1: 1 h 2: water; hydrogen bromide / 15 h / Reflux 3: L-(+)-tartaric acid / 75 °C View Scheme
参考文献
Investigational New Drugs, , vol. 28, # 4 p. 454 - 465
反应条件
optical resolution with chiral tartaric acid;
参考文献
Bioorg. Med. Chem. Lett., , vol. 14, # 12 p. 3251 - 3256
反应条件
1.1: triethylamine / methanol / 1.5 h / 10 - 20 °C 2.1: sodium tetrahydroborate; boron trifluoride diethyl etherate / tetrahydrofuran / 4 h / 0 - 50 °C 2.2: 0.17 h / 10 °C 3.1: 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 ;
反应条件
1: With sulfuric acid in methanol T=0°C; 1.5 h; 2: With sodium tetrahydroborate in methanol T=0 - 25°C; 1.83333 - 1.91667 h;
参考文献
ALEMBIC LIMITED
Patent: WO2006/3677 A1, 2006 ;
Location in patent: Page/Page column 10; 18-19 ;