Table 2.

Exploration and Optimization of Oridonin-Based Aziridination^a

entries	DPH amount (equiv)	catalystb	temp/time	recovery of 21c	yield of productsc
1	2.2	Rh2(esp)2	rt./12 h	trace	22 (69%)
2	2.2	Rh2(OAc)4	rt./12 h	trace	22 (58%)
3	2.2	Rh2(TPA)4	rt./12 h	>80%	22 (trace)
4	2.2	Rh2(R-DOSP)4	rt./12 h	>80%	22 (NA)d
5	2.2	Rh2(S-DOSP)4	rt./12 h	>80%	22 (NA)
6	1.2	Rh2(esp)2	rt./12 h	18%	22 (54%)
7	1.5	Rh2(esp)2	rt./12 h	5%	22 (66%)
8	4.4	Rh2(esp)2	rt./24 h	NA	22 (71%)
					23 (NA)
9	4.4	Rh2(esp)2	50°C/24 h	NA	22 (66%)
					23 (NA)
10	4.4	Rh2(esp)2	reflux/48 h	NA	22 (56%)
					23 (NA)

^aAll reaction conditions in this table were performed, utilizing 21 as the substrate.

^bThe equivalent of catalyst is 5%.

^cThe data were based on isolated yields.

^dNA: not available.