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. 2017 May 15;25(10):2730–2742. doi: 10.1016/j.bmc.2017.03.041

Scheme 2.

Scheme 2

Synthesis of first generation compounds 4aj. Reagents and conditions: (a) HATU, TEA, CH2Cl2, r.t., 5 h.; (b) TFA/CH2Cl2 95:5, r.t., 2 h.; (c) LiOH, THF/H2O 4:1, r.t., overnight.