反应条件
1.1: 98 percent / oxalyl chloride; DMSO; Et3N / CH2Cl2 / 1 h / -78 °C
2.1: 65 percent / NaHSO3 / H2O; methanol / 16 h / Heating
3.1: 78 percent / aq. HCl; AcOH / 18 h / 80 °C
4.1: H2; AcOH / Pd(OH)2/C / methanol / 18 h / 2585.74 Torr
5.1: 4.07 g / K2CO3 / dimethylformamide / 19 h
6.1: 51 percent / KMnO4; aq. KOH / 1.5 h / 60 - 90 °C
7.1: 85 percent / EDAC; HOBT; TEA / dimethylformamide / 20 °C
8.1: pyridine; trifluoroacetic anhydride / tetrahydrofuran / 1 h
8.2: 92 percent / aq. KOH / methanol / 18 h / 20 °C
View Scheme
参考文献
Augeri, David J.; Robl, Jeffrey A.; Betebenner, David A.; Magnin, David R.; Khanna, Ashish; Robertson, James G.; Wang, Aiying; Simpkins, Ligaya M.; Taunk, Prakash; Huang, Qi; Han, Song-Ping; Abboa-Offei, Benoni; Cap, Michael; Xin, Li; Tao, Li; Tozzo, Effie; Welzel, Gustav E.; Egan, Donald M.; Marcinkeviciene, Jovita; Chang, Shu Y.; Biller, Scott A.; Kirby, Mark S.; Parker, Rex A.; Hamann, Lawrence G.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 15 p. 5025 - 5037
