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. Author manuscript; available in PMC: 2021 Mar 12.
Published in final edited form as: J Med Chem. 2019 Sep 26;63(5):2139–2180. doi: 10.1021/acs.jmedchem.9b00826

Scheme 1.

Scheme 1.

First-generation synthetic route to aminopyrazole/isoindoline resorcylate amides Conditions: a) POCl3, DMF, 100 °C; b) BBr3, CH2Cl2, −78 °C to RT; c) MOMCl, DIPEA, DMF; d) NaOCl2, NaH2PO4•H2O, 2-methyl-2-butene, THF/tBuOH/H2O; e) isoindoline•HCl, HATU, Et3N, THF/CH2Cl2; f) tBuXphos Pd G1 (10 mol%), tBuXPhos (10 mol%), NaOtBu, tBuOH, or Pd2(dba)3 (4 mol%), Xantphos (8 mol%), NaOPh, dioxane, 60 °C to 120 °C, or Pd2(dba)3 (10 mol%), Xantphos (10 mol%), NaOPh, dioxane, 170 °C, microwave; g) HCl, methanol, 50 °C.