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. Author manuscript; available in PMC: 2023 Jan 27.
Published in final edited form as: J Med Chem. 2021 Oct 20;65(2):1370–1383. doi: 10.1021/acs.jmedchem.1c00848

Scheme 4.

Scheme 4.

Preparation of irreversible binding inhibitor 1 a

aReagents and conditions: (i) a) N-(3-Bromo-4-methoxyphenyl) acrylamide, Cs2CO3, BrettPhos Pd G3, 1,4-dioxane/t-BuOH, rf, b) TFA/DCM 5 %, 41 %; (ii) 17, (COCl)2, DMF cat., Et3N, THF, rt, 70 %; (iii) TFA, DCM, H2SO4, 1,4-dioxane, rt, 80 %.