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. Author manuscript; available in PMC: 2021 Feb 10.
Published in final edited form as: Angew Chem Int Ed Engl. 2020 Jan 8;59(7):2674–2678. doi: 10.1002/anie.201913730

Table 1:

Condition screening for a Pd-based cyclization–functionalization.[a]

graphic file with name nihms-1561410-t0004.jpg
Entry Ligand (loading) Acetate source Yield [%][b]
1 Trixiephos (30 mol%) NaOAc –
2 Trixiephos (30 mol%) KOAc 4
3 Trixiephos (30 mol%) n-Bu4OAc 61
4 Trixiephos (15 mol%) n-Bu4OAc 86
5 Johnphos (15 mol%) n-Bu4OAc 76
6 t-BuDavephos (15 mol%) n-Bu4OAc 82
7 t-BuXantphos (15 mol%) n-Bu4OAc 52
8 dtbpf (15 mol%) n-Bu4OAc 22
9 t-BuMephos (15 mol%) n-Bu4OAc 95
10[c] t-BuMephos (15 mol%) n-Bu4OAc 96 (95)
[a]

Reaction conditions unless otherwise noted: 17 (0.2 mmol), Pd-(OAc)2 (0.02 mmol), ligand (0.03 mmol), acetate source (0.6 mmol), toluene (2 mL), 130°C.

[b]

Yields were determined by 1H NMR using 1,3,5-trimethoxybenzene as an internal standard with the yield in parentheses reflecting the yield of isolated product.

[c]

Reaction temperature was 90°C.