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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 2.

Scheme 2.

Early exploration of amide SAR using first-generation synthetic route Conditions: a) HNR4R5, HATU, Et3N, THF/CH2Cl2; b) 10a, Pd2(dba)3 (4 mol%), Xantphos (10 mol%), NaOPh, dioxane, 170 °C, microwave; c) HCl, methanol, 50 °C.