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. 2021 Jun 22;12(27):9475–9484. doi: 10.1039/d1sc03007h

Scope of the coupling conditions optimised by factorial design. Conditions: 2 (5 nmol), amine (0.5 M), 2,6-lutidine (1.5 M), DIC (0.5 M), HOAt (0.5 M), 4.5% TPGS, 30 μl total volume, 45 °C, 3 h. Reactions proceeded to full conversion. Percentage of the by-product shown in parentheses.

Amine % Conversion % Product Amine % Conversion % Product
1 graphic file with name d1sc03007h-u17.jpg 100 100 18 graphic file with name d1sc03007h-u18.jpg 100 100
2 graphic file with name d1sc03007h-u19.jpg 100 100 19 graphic file with name d1sc03007h-u20.jpg 100 95
3 graphic file with name d1sc03007h-u21.jpg 100 100 20 graphic file with name d1sc03007h-u22.jpg 100 86
4 graphic file with name d1sc03007h-u23.jpg 100 96 21 graphic file with name d1sc03007h-u24.jpg 100 85
5 graphic file with name d1sc03007h-u25.jpg 100 100 22 graphic file with name d1sc03007h-u26.jpg 100 58
6 graphic file with name d1sc03007h-u27.jpg 100 98 23 graphic file with name d1sc03007h-u28.jpg 98 84
7 graphic file with name d1sc03007h-u29.jpg 100 100 24 graphic file with name d1sc03007h-u30.jpg 91 86
8 graphic file with name d1sc03007h-u31.jpg 100 100 25 graphic file with name d1sc03007h-u32.jpg 98 94
9 graphic file with name d1sc03007h-u33.jpg 100 100 26 graphic file with name d1sc03007h-u34.jpg 93 93
10 graphic file with name d1sc03007h-u35.jpg 100 100 27 graphic file with name d1sc03007h-u36.jpg 98 98
11 graphic file with name d1sc03007h-u37.jpg 100 100 28 graphic file with name d1sc03007h-u38.jpg 98 98
12 graphic file with name d1sc03007h-u39.jpg 100 100 29 graphic file with name d1sc03007h-u40.jpg 94 94
13 graphic file with name d1sc03007h-u41.jpg 100 100 30 graphic file with name d1sc03007h-u42.jpg 98 97
14 graphic file with name d1sc03007h-u43.jpg 100 100 31 graphic file with name d1sc03007h-u44.jpg 100 87
15 graphic file with name d1sc03007h-u45.jpg 100 100 32 graphic file with name d1sc03007h-u46.jpg 100 95
16 graphic file with name d1sc03007h-u47.jpg 100 100 33 graphic file with name d1sc03007h-u48.jpg 100 35
17 graphic file with name d1sc03007h-u49.jpg 100 100 34 graphic file with name d1sc03007h-u50.jpg 100 58