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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 3.

Scheme 3.

Preparation of reversible binding inhibitors 2a, 2b and 2c a

aReagents and conditions: (i) 16, TBTU, Et3N, DMF, rt; 17/18 (COCl)2, DMF cat., Et3N, THF, rt, 60 %/87 %; (ii) NaHCO3 (aq), MeOH and TFA, DCM, rt or TFA, DCM, rt and TBAF, THF, rt, 48–57 %.