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Synthesis of sEHI amides 6a–h from polycyclic amines 2a–e. (a) EDC·HCl, HOBt, Et3N, EtOAc, rt, 24 h (4a–b, 4d); (b) HATU, DIPEA, DMF, rt, overnight (4c, 4e, 6g–h); (c) HCl/Dioxane, rt, 2 h (5a–e); (d) acetyl chloride, Et3N, DCM, 0 °C to rt, overnight (6a); (e) propane-2-sulfonyl chloride, Et3N, DCM, 0 °C to rt, overnight (6b–f).
