C-[4-(3,4-二氯-苄基)-吗啉-2-基]-甲胺双盐酸盐合成路线 （共 8 条）
反应条件
1: T=80°C; 3 h;
2: With sulfuric acid
T=150°C; 24 h;
3: With sodium hydroxide in water
pH=~ 12; Product distribution / selectivity;
参考文献
GLAXO GROUP LIMITED
Patent: WO2003/82834 A2, 2003 ;
Location in patent: Page/Page column 17 ;
WO 03/082834 A2
参考文献
Wilkinson, Mark C.
Tetrahedron Letters, 2005 , vol. 46, # 28 p. 4773 - 4775
反应条件
1: H2, AcOH / 10percent Pd/C / ethanol / 60 °C
2: K2CO3, KI / butan-2-one / 17 h / Heating
3: 10percent HCl / 4 h / Heating
View Scheme
参考文献
Kato; Morie; Kon; Yoshida; Karasawa; Matsumoto
Journal of Medicinal Chemistry, 1991 , vol. 34, # 2 p. 616 - 624
反应条件
1: 80 percent / phenyl 'Trost' ligand / Pd2dba3 / tetrahydrofuran / 50 °C
2: 83 percent / OsO4; NMO / acetone; H2O
3: NaIO4 / tetrahydrofuran; H2O
4: NaBH4
5: TPP; DIAD / tetrahydrofuran
6: 97 percent / aq. HNMe2
View Scheme
参考文献
Wilkinson, Mark C.
Tetrahedron Letters, 2005 , vol. 46, # 28 p. 4773 - 4775
反应条件
1: K2CO3, KI / butan-2-one / 17 h / Heating
2: 10percent HCl / 4 h / Heating
View Scheme
参考文献
Kato; Morie; Kon; Yoshida; Karasawa; Matsumoto
Journal of Medicinal Chemistry, 1991 , vol. 34, # 2 p. 616 - 624
反应条件
1: 83 percent / OsO4; NMO / acetone; H2O
2: NaIO4 / tetrahydrofuran; H2O
3: NaBH4
4: TPP; DIAD / tetrahydrofuran
5: 97 percent / aq. HNMe2
View Scheme
参考文献
Wilkinson, Mark C.
Tetrahedron Letters, 2005 , vol. 46, # 28 p. 4773 - 4775
反应条件
hydrogenchloride
4 h; Heating;
参考文献
Kato; Morie; Kon; Yoshida; Karasawa; Matsumoto
Journal of Medicinal Chemistry, 1991 , vol. 34, # 2 p. 616 - 624
反应条件
Resolution of racemate; Purification / work up;
参考文献
GLAXO GROUP LIMITED
Patent: WO2003/82862 A1, 2003 ;
Location in patent: Page/Page column 27-28 ;
WO 03/082862 A1
