4-[6-[(6-溴-8-环戊基-7,8-二氢-5-甲基-7-氧代吡啶并[2,3-d]嘧啶-2-基)氨基]-3-吡啶基]-1-哌嗪羧酸叔丁酯合成路线 (共 6 条)
反应条件
in toluene
7 h; Heating;
参考文献
Barvian, Mark; Booth, Richard John; Ouin III, John; Thomas Repine, Joseph; Sheehan, Derek J.; Toogood, Peter Laurence; Vanderwel, Scott Norman; Zhou, Hairong
Patent: US2003/149001 A1, 2003 ;
US 20030149001 A1
反应条件
1: 190.93 g / aq. NaHCO3 / tetrahydrofuran / 3 h
2: 83 percent / H2 / Raney Nickel / methanol / 5 h / 2585.74 Torr
3: 38 percent / toluene / 7 h / Heating
View Scheme
参考文献
Toogood, Peter L.; Harvey, Patricia J.; Repine, Joseph T.; Sheehan, Derek J.; VanderWel, Scott N.; Zhou, Hairong; Keller, Paul R.; McNamara, Dennis J.; Sherry, Debra; Zhu, Tong; Brodfuehrer, Joanne; Choi, Chung; Barvian, Mark R.; Fry, David W.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 7 p. 2388 - 2406
反应条件
1: 83 percent / H2 / Raney Nickel / methanol / 5 h / 2585.74 Torr
2: 38 percent / toluene / 7 h / Heating
View Scheme
参考文献
Toogood, Peter L.; Harvey, Patricia J.; Repine, Joseph T.; Sheehan, Derek J.; VanderWel, Scott N.; Zhou, Hairong; Keller, Paul R.; McNamara, Dennis J.; Sherry, Debra; Zhu, Tong; Brodfuehrer, Joanne; Choi, Chung; Barvian, Mark R.; Fry, David W.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 7 p. 2388 - 2406
反应条件
1: tetra-n-butylammonium iodide; K2CO3 / dimethylsulfoxide / 80 - 100 °C
2: 190.93 g / aq. NaHCO3 / tetrahydrofuran / 3 h
3: 83 percent / H2 / Raney Nickel / methanol / 5 h / 2585.74 Torr
4: 38 percent / toluene / 7 h / Heating
View Scheme
参考文献
Toogood, Peter L.; Harvey, Patricia J.; Repine, Joseph T.; Sheehan, Derek J.; VanderWel, Scott N.; Zhou, Hairong; Keller, Paul R.; McNamara, Dennis J.; Sherry, Debra; Zhu, Tong; Brodfuehrer, Joanne; Choi, Chung; Barvian, Mark R.; Fry, David W.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 7 p. 2388 - 2406
反应条件
1: 2-benzenesulfonyl-3-phenyloxaziridine / CH2Cl2 / 18 h / 20 °C
2: 38 percent / toluene / 7 h / Heating
View Scheme
参考文献
Toogood, Peter L.; Harvey, Patricia J.; Repine, Joseph T.; Sheehan, Derek J.; VanderWel, Scott N.; Zhou, Hairong; Keller, Paul R.; McNamara, Dennis J.; Sherry, Debra; Zhu, Tong; Brodfuehrer, Joanne; Choi, Chung; Barvian, Mark R.; Fry, David W.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 7 p. 2388 - 2406
反应条件
in toluene
25 h; Heating / reflux; Product distribution / selectivity;
参考文献
PFIZER PRODUCTS INC.
Patent: WO2008/32157 A2, 2008 ;
Location in patent: Page/Page column 24 ;