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. Author manuscript; available in PMC: 2023 Feb 24.
Published in final edited form as: J Med Chem. 2022 Feb 4;65(4):3644–3666. doi: 10.1021/acs.jmedchem.1c02165

Scheme 4. Syntheses of Linkers 66–69 and 82–87a.

Scheme 4.

aReaction conditions: (a) EDCI, HOAt, NMM, DMSO, rt, 12 h; (b) NMP, DIPEA, MW, 100 °C, 1 h; (c) TFA, DCM, rt, 30 min; (d) NaHCO3, KI, DMF, 60 °C, overnight; (e) Pd(PPh3)2Cl2, CuI, NEt3, DMF, 70 °C, 2 h; and (f) Pd/C, H2, MeOH, rt, 1 h.