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. 2020 Mar 24;11(5):825–831. doi: 10.1021/acsmedchemlett.9b00633

Scheme 1. Synthesis of Compounds 216.

Scheme 1

Reagents and conditions: (a) NH2R1, HOBt, DCC, DMF, rt for 17 and 21. (b) NH2R1, HOBt, EDC.HCl, DMF, rt for 1820 and 2225. (c) R2B(OH)2, Pd(dppf)Cl2, Cs2CO3, dioxane/water, MW 130 °C for 210. (d) R2B(OH)2 or R2Br, Pd(dppf)Cl2, CsF, dioxane/water 100 °C for 1115. (e) bis(pinacolato)diboron, Pd(dppf)Cl2, KOAc, dioxane, 100 °C. (f) R2Br, Pd(PPh3)4, Na2CO3, DMF/water, 100 °C for 16.