Scheme 4. Synthesis of RB-044–RB-050 from 4-Iodobenzoic Acid.
Reagents and conditions: (a) 1-octyne, Pd(PPh3)4, CuI, Et3N, 60 °C, 12 h; (b) Pd/C, H2, EtOAc, 12 h, rt; (c) (i) SOCl2, CH2Cl2, reflux, 12 h; (ii) cyclic amine, K2CO3, MeCN, 50 °C, 12 h.
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