Table 1.
Conditions: 1a (0.1 mmol, 1.0 equiv), methyl 4-iodobenzoate (2.0 equiv), Pd(OAc)2 (10 mol%), TDG1 (glycine, 30 mol%), L12 (60 mol%), AgTFA (3.0 equiv) and ClCH2COOH (1.5 equiv) in HFIP (0. 5 mL), 120°C, under air, 48 h.
Yield determined by 1H NMR; CH2Br2 as internal standard.
Loading that gave the highest yield within a serial of concentrations.
Ratio of mono:di.