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. 2020 Dec 2;5(49):32067–32075. doi: 10.1021/acsomega.0c05099

Table 1. Reaction Optimization Conditions.

graphic file with name ao0c05099_0010.jpg

entry equiv 14 (x) cosolvent, (vol) time (h) temp. (°C) conversion (area %)a
1 1.2 (0) 2 100 63
2 1.2 MeCN, (10) 19 22 88
3 1.2 MeCN, (10) 3 40 90
4 1.2 MeOH, (10) 3 40 84
5 1.2 DMSO, (10) 3 40 87
6 1.2 MeTHF, (10) 3 40 79
7 1.2 DCM, (10) 3 40 77
8 1.2 H2O, (10)b 3 40 66
9 1.05 MeCN, (5) 3 35 90
9b 28 35 89
10 1.05 MeCN, (5) 3 35 90 (80)c
a

UPLC-UV percent area at 269 nm.

b

Total water was 20 vol.

c

Isolated yield.