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. Author manuscript; available in PMC: 2023 Oct 13.
Published in final edited form as: J Med Chem. 2022 Sep 20;65(19):13198–13215. doi: 10.1021/acs.jmedchem.2c00998

Scheme 1.

Scheme 1.

(a) LDA, THF or ether, −78 °C, 30 min then ethyl trifluoroacetate 2h at rt; (b) ethyl 2-hydrazinoacetate, isopropanol or toluene, 75 °C, 2h;(c) LiOH, H2O, 70 °C, 1h (d) N-Me aniline, DIPEA, HATU or T3P, DMF or THF rt.