Table 1. Optimization of Reaction Conditions.

entryc	conc (i–ii M)	time (i, ii min)	yielda (%)
1	0.3	30, 30	43b
2	0.3	30, 40	50b
3	0.3–0.1	30, 40	58b
4	0.3–0.08	30, 40	66b
5	0.3–0.05	30, 40	34b,d

^aFinal isolated yield over two reactions after flash chromatography.

^bAziridine opening: 1 (1.0 equiv) and 2 (1.05–1.3 equiv) in DMF at 130 °C. S_NAr: Cs₂CO₃ (2.5 equiv) in DMF at 150 °C.

^cReactions were monitored by TLC.

^dReaction was run only once at 0.05.