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Synthesis of Designed Protease Inhibitors III and IVa
a Reagents and conditions: (a) i-PrOH, 80 °C, 24 h; (b) Pd/C, MeOH, rt, overnight; (c) acid A3, EDCI, HOBt, DIPEA, DMF–CH2Cl2 (1:1), 0 °C to rt, 12 h (d) TFA, CH2Cl2, 1 h; (e) acid 11a, (COCl)2, rt, overnight; (f) Et3N, THF, 0 °C to rt, 8 h.
