Scaffold oriented synthesis. Part 1: design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors

I Akritopoulou-Zanze, D Darczak, K Sarris…

文献索引：Akritopoulou-Zanze, Irini; Darczak, Daria; Sarris, Kathy; Phelan, Kathleen M.; Huth, Jeffrey R.; Song, Danying; Johnson, Eric F.; Jia, Yong; Djuric, Stevan W. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 1 p. 96 - 99

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被引用次数: 20

摘要

... PMBCl, K 2 CO 3 , DMF, 120 °C, 1 h; PG = BPMPM, BPMPMCl, 14 Et 3 N, THF, rt, 1 h; (c) Mercapto-acetic acid methyl ester, Na 2 CO 3 , MeOH, reflux; (d) PG = PMB, 1:1 TFA/CH 2 Cl 2 , 120 °C, 20 min, microwave (CEM, 300 W, ramp time 1 min), 59%; (e) PG = BPMPM, 4 M HCl in dioxane, rt, 1 h, 60%; (f) Boc 2 O, Et 3 N, DMAP, MeCN, 3 h, 66%; (g) NBS, (PhCO 2 ) 2 , CCl 4 , reflux, 6 h, 24%; (h) R 1 R 2 NH, EtOH; (i) 1:1 TFA/CH 2 Cl 2 , 24–84% in two steps. ...