Table 2:

1,4-Diazepine formation reaction with 2.

Entry	a)	b)	Yield %	% ee
1a	HCl (g), saturated, rtd, 18 h	MeOH / H2O (9 : 1), 0.1 eq NaOH, rtd, 10 h	8212	99.512
2b	HCl in dioxane, 4 eq, rtd, 4 h	MeOH / H2O (9 : 1), 0.1 eq NaOH, rtd, 48 h	84	53.9
3c	HCl in dioxane, 4 eq, rtd, 4 h	MeOH / H2O (9 : 1), 1 eq NaOH, rtd, 12 h	50	0
4c	HCl in dioxane, 4 eq, rtd, 4 h	Toluene, 60 °C, 4 h	48	99.2

^a60 mM scale

^b116 mM scale

^c122 mM scale

^drt = room temperature