Table 1: Different coupling condition for amide synthesis.

Entry Starting materialReagents/conditionsProduct (isolated yield%)

14aHA1.2 eq. DCC, cat. DMAP, CH2Cl2, r.t., 8 h46
24aHA1 eq. EDC, cat. DMAP, CH2Cl2 r.t., 8 h36
34aHA1.1 eq. EDC, cat. DMAP, CH2Cl2 r.t., 12 h70
44aHA1.3 eq. EDC, cat. DMAP, CH2Cl2 r.t., 12 h76
55aHA1.3 eq. EDC, cat. DMAP, CH2Cl2 r.t., 12 h61
66aHA1.3 eq. EDC, cat. DMAP, CH2Cl2 r.t., 18 h79