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. 2020 Oct 13;11(12):2382–2388. doi: 10.1021/acsmedchemlett.0c00267

Scheme 1. Synthesis of Picolinic Acid Derivatives.

Scheme 1

Reagents and conditions: (a) 2.6 M Br2 in AcOH, 2 M H2SO4, rt, 4–72 h, 51–55%; (b) ArCOCl, Et3N or i-Pr2EtN, THF or CH3CN, rt to 150 °C, 30–89%; (c) PhB(OH)2, Na2CO3, Pd(PPh3)2Cl2, 10:1 CH3CN/H2O, 100 °C, 0.5 h, 67%; (d) 1.3 M aq LiOH, 3:2 THF/H2O, rt, 12–48 h, 31–93%.