4-(1-氰基-2-乙氧基-2-氧代乙基)-4-苯基哌啶-1-羧酸叔丁酯合成路线 （共 5 条）
反应条件
1: With copper(l) iodide in tetrahydrofuran
T=0 - 23°C; 0.666667 h;
2: With hydrogenchloride in tetrahydrofuran; water
T=0°C; pH=5;
参考文献
GLAXO GROUP LIMITED
Patent: WO2004/5256 A2, 2004 ;
Location in patent: Page 47 ;
WO 2004/005256 A2
反应条件
1: bromobenzene With magnesium in tetrahydrofuran
T=20°C;
2: ethyl cyano(1-Boc-4-piperidinylidene)acetate With copper(l) iodide in tetrahydrofuran
T=0 - 20°C; Grignard addition;
参考文献
Chauder, Brian A.; Boros, Eric E.; Du, Kien S.; Kazmierski, Wieslaw M.; Koble, Cecilia S.; Thompson, James B.; Tabet, Elie A.
Synthetic Communications, 2006 , vol. 36, # 3 p. 279 - 284
反应条件
1.1: 100 percent / NH4OAc; AcOH; benzene
2.1: magnesium / tetrahydrofuran / 20 °C
2.2: copper(I) iodide / tetrahydrofuran / 0 - 20 °C
View Scheme
参考文献
Chauder, Brian A.; Boros, Eric E.; Du, Kien S.; Kazmierski, Wieslaw M.; Koble, Cecilia S.; Thompson, James B.; Tabet, Elie A.
Synthetic Communications, 2006 , vol. 36, # 3 p. 279 - 284
反应条件
1.1: 100 percent / NH4OAc; AcOH; benzene
2.1: magnesium / tetrahydrofuran / 20 °C
2.2: copper(I) iodide / tetrahydrofuran / 0 - 20 °C
View Scheme
参考文献
Chauder, Brian A.; Boros, Eric E.; Du, Kien S.; Kazmierski, Wieslaw M.; Koble, Cecilia S.; Thompson, James B.; Tabet, Elie A.
Synthetic Communications, 2006 , vol. 36, # 3 p. 279 - 284
反应条件
1: 4-(1-cyano-1-ethoxycarbonyl-methyl)-4-phenyl-piperidine-1-carboxylic acid tert-butyl ester With sulfuric acid; water; acetic acid
T=140°C; 12 h;
2: di-tert-butyl dicarbonate With sodium hydroxide in water
T=20°C; pH=8; 48 h;
3: With hydrogenchloride in water
T=0°C; pH=6 - 7;
参考文献
GLAXO GROUP LIMITED
Patent: WO2004/5256 A2, 2004 ;
Location in patent: Page 47-48 ;
WO 2004/005256 A2
