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. 2020 Jul 29;11(33):8779–8784. doi: 10.1039/d0sc02881a

Conditions optimizationa.

graphic file with name d0sc02881a-u1.jpg
Entry Variation from standard conditions 4Aa b/%
1 None 88
2 P(p-anisyl)3 instead of L1 81
3 PPh3 instead of L1 58
4 P(C6F5)3 instead of L1 0
5 DPEphos (10 mol%) instead of L1 92
6 Without L1 0
7 LiOtBu instead of NaH 2
8 Cs2CO3 instead of NaH 0
9 Without 3 Å MS 71
10 3a′ was used instead of 3ac 62
11 Cyclohexane instead of toluene 54
a

Conditions: 1A (0.20 mmol), 2 (0.20 mmol), 3a (0.20 mmol), Pd(OAc)2 (5.0 mol%), L1 (20 mol%), NaH (1.0 equiv.), 3 Å MS (50 mg), toluene (1.0 mL), 60 °C, 12 h.

b

NMR yield.

c

Without NaH and 3 Å MS at 70 °C.