Skip to main content
. 2023 Apr 26;66(9):6391–6402. doi: 10.1021/acs.jmedchem.3c00415

Scheme 10. Synthesis of 2528.

Scheme 10

Reagents and conditions: (a) NaH, Tf2O, 0 °C to rt, 1 h, 70%; (b) HCOONa, DMF, LiCl, Ac2O, DIPA, XPhos-Pd-G2, 0 °C then 50 °C, 18 h, 57%; (c) EDC·HCl, CHCl3, rt, 2 h, then 33d, NEt3, reflux, 18 h, 13%; (d) LiOH, THF/H2O, rt, 20 min, 95%; (e) XPhos-Pd-G2, Cs2CO3, PhCH3/EtOH/DMF/H2O, 100 °C, 18 h, 59–99%.