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 |
![]() |
100 | 100 | 18 |
![]() |
100 | 100 |
2 |
![]() |
100 | 100 | 19 |
![]() |
100 | 95 |
3 |
![]() |
100 | 100 | 20 |
![]() |
100 | 86 |
4 |
![]() |
100 | 96 | 21 |
![]() |
100 | 85 |
5 |
![]() |
100 | 100 | 22 |
![]() |
100 | 58 |
6 |
![]() |
100 | 98 | 23 |
![]() |
98 | 84 |
7 |
![]() |
100 | 100 | 24 |
![]() |
91 | 86 |
8 |
![]() |
100 | 100 | 25 |
![]() |
98 | 94 |
9 |
![]() |
100 | 100 | 26 |
![]() |
93 | 93 |
10 |
![]() |
100 | 100 | 27 |
![]() |
98 | 98 |
11 |
![]() |
100 | 100 | 28 |
![]() |
98 | 98 |
12 |
![]() |
100 | 100 | 29 |
![]() |
94 | 94 |
13 |
![]() |
100 | 100 | 30 |
![]() |
98 | 97 |
14 |
![]() |
100 | 100 | 31 |
![]() |
100 | 87 |
15 |
![]() |
100 | 100 | 32 |
![]() |
100 | 95 |
16 |
![]() |
100 | 100 | 33 |
![]() |
100 | 35 |
17 |
![]() |
100 | 100 | 34 |
![]() |
100 | 58 |