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. 2021 Dec 24;14(1):33. doi: 10.3390/pharmaceutics14010033

Table 1.

Microwave-assisted amide synthesis 1.

Entry Nomenclature X Y Yield (%) 2
1 8a CH2 H 50
2 8b N-Boc H 70
3 8c O H 43
4 8d S H 82
5 8e CH2 F 19
6 8f N-Boc F 62
7 8g O F 52
8 8h S F 42
9 8i CH2 Cl 19
10 8j N-Boc Cl 69
11 8k O Cl 27
12 8l S Cl 51
13 8m CH2 Br 27
14 8n N-Boc Br 56
15 8o O Br 66
16 8p S Br 83 (44) 3
17 8q CH2 CH3 30
18 8r N-Boc CH3 57
19 8s O CH3 31
20 8t S CH3 57

1 Reaction conditions: 3 (0.65 mmol), 7 (0.5 mmol), HATU (0.5 mmol), EDC (0.5 mmol), Py (0.5 mmol), solvent (8 mL), N2 atmosphere, 70 °C, MW, 30 min. 2 Yields of isolated products after column chromatographic. 3 Yield using 2-MeTHF as solvent under optimized conditions.