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. 2022 Apr 28;65(17):11574–11606. doi: 10.1021/acs.jmedchem.2c00252

Scheme 4. Synthesis of Derivatives 12a12h.

Scheme 4

Reagents and conditions: (a) NaH 60% mineral oil, TFAA, dry THF, r.t., 16 h (33–53%); (b) EDC hydrochloride, TEA, DCM, r.t., 18 h (72–81%); (c) DCM/TFA, 1:1, r.t., 2 h (74–80%).