Table 1 Reaction optimization


Entry	Variation from the entry “standard conditions”	Yield of 3a (%)^a
1	none	96 (94)^b
2	K₂CO₃ instead of Cs₂CO₃	90
3	KOAc instead of Cs₂CO₃	<5
4	t-BuOK instead of Cs₂CO₃	<5
5	Et₃N instead of Cs₂CO₃	57
6	In dark	95
7	CH₂Cl₂	<5
8	MeCN	70
9	DMF	56
10	under air	<5

^aReaction conditions: 1a (0.3 mmol, 3.0 equiv), 2a (0.1 mmol), and Cs₂CO₃ (0.15 mmol, 1.5 equiv) in MeOH (1.0 mL) at 22 °C for 2 h. Yield was determined by ¹H NMR spectroscopy in the presence of CH₂Br₂ as an internal standard. ^bIsolated yield.

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