Scheme 1. Synthesis of Compounds 2–16.
Reagents and conditions: (a) NH2R1, HOBt, DCC, DMF, rt for 17 and 21. (b) NH2R1, HOBt, EDC.HCl, DMF, rt for 18–20 and 22–25. (c) R2B(OH)2, Pd(dppf)Cl2, Cs2CO3, dioxane/water, MW 130 °C for 2–10. (d) R2B(OH)2 or R2Br, Pd(dppf)Cl2, CsF, dioxane/water 100 °C for 11–15. (e) bis(pinacolato)diboron, Pd(dppf)Cl2, KOAc, dioxane, 100 °C. (f) R2Br, Pd(PPh3)4, Na2CO3, DMF/water, 100 °C for 16.
