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. 2022 Jan 27;24(5):1127–1131. doi: 10.1021/acs.orglett.1c04045

Table 1. Optimization Tablea.

graphic file with name ol1c04045_0007.jpg

entry variations from standard conditionsa yield (%)b of 3aa
1 none 97 (96)c
2 without PPh3 NR
3 BINAP instead of PPh3 NR
4 toluene instead of CHCl3 60
5 DCM instead of CHCl3 78
6 EtOAc instead of CHCl3 64
7 CDCl3 instead of CHCl3 93
8 1 equiv of 1a 46
9 2 equiv of 1a 82
10 0.2 mmol 1a and 2 equiv of 2a 20
a

Unless otherwise noted, the standard reaction conditions were as follows: 1a (0.6 mmol), 2a (0.2 mmol), solvent (0.5 mL).

b

The yield was determined by 1H NMR analysis of the crude reaction mixture using 1,3,5-trimethoxybenzene as an internal standard.

c

Isolated yield.