. 2020 Apr 16;5(16):9614–9623. doi: 10.1021/acsomega.0c01104

Table 1. Optimization of Reaction Conditions^a.

					yield (%)
entry	R₁	catalyst	base	solvent	3a/4a	5a/6a
1^b	H	DMAP	Et₃N	CH₂Cl₂	9	33
2^b	H		Et₃N	CH₂Cl₂	9	13
3^b	H	DMAP		CH₂Cl₂		79
4^b	H			CH₂Cl₂	10	47
5^b	H	TBD		CH₂Cl₂		NR^e
6^b	H	DBU		CH₂Cl₂		NR^e
7^b	H	DABCO		CH₂Cl₂		36
8^b	H	DMAP		THF		58
9^b	H	DMAP		DMF		61
10^b	H	DMAP		CH₃CN		94
11^b	CH₃	DMAP		CH₃CN	46	46
12^c	CH₃	DMAP		CH₃CN	21	59
13^d	CH₃	DMAP		CH₃CN		92

All reactions were conducted using 1a/2a (1 mmol, 1.0 equiv), (Boc)₂O (1.5 mmol, 1.5 equiv), catalyst (0.1 mmol, 0.1 equiv), solvent (3 mL), isolated yield.

The reaction was run at room temperature for 12 h.

The reaction was run at reflux for 12 h.

The reaction was run under the microwave (MW) condition for 30 min.

No reaction.

Table 1. Optimization of Reaction Conditionsa.

Table 1. Optimization of Reaction Conditions^a.