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. 2021 Nov 30;64(24):17901–17919. doi: 10.1021/acs.jmedchem.1c01212

Scheme 3. Reagents and Conditions: (a) NaH (60% Dispersion in Mineral Oil), 0 °C, DMF and Then 4 h, rt; (b) Anhydrous CH2Cl2/TFA (8:2, v/v, 20 mL), rt, 1 h; (c) ACy (i–iv and vii–viii), TBTU (1.1 equiv), HOBt (1.1 equiv), DIPEA, DMF, Overnight, rt; and (d) (1) SOCl2 (10 equiv), Anhydrous CH2Cl2, Reflux, 1 h and (2) ACy (v and vi, 2 equiv), Anhydrous Tetrahydrofuran, Overnight, rt.

Scheme 3