Table 1.

Rh-catalyzed intramolecular aziridination.

entrya	substrateb	product		yield
1				64c
2			R = Troc	98
			R = Boc	78
3				94
4d			R = Troc	86	3:1 dr
			R = Boc	82	3:1 dr
			R = Mbs	93	13:1 dr
5				82
6				65
7				51

^aReactions conducted in ⁱPrOAc using 2 mol % Rh₂(esp)₂, 2.3 equiv of MgO and 1.1 equiv of PhI(OAc)₂.

^bSubstrates were prepared using either Mitsunobu or π-allyl Pd chemistry in yields ranging from 60–99%. See supporting information for details.

^cIsolated yield of this aziridine was reduced due to difficulties associated with its purification. See supporting information for details.

^dProduct diastereomeric ratios determined by 1H NMR integration.