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. 2025 Jan 15;30(2):317. doi: 10.3390/molecules30020317

Table 2.

Synthesis of 1,5-disubstituted triazoles 3 a.

graphic file with name molecules-30-00317-i002.jpg
Entry 3 R1 R2 R3 R4 Yield (%) b
1 3a H H H H 72
2 3b Br H H H 85
3 3c NO2 H H H 59
4 3d H H Me H 60
5 3e H H CF3 H 61
6 3f H H F H 51
7 3g H H Cl H 51
8 3h H H Br H 66
9 3i H H OMe H 60
10 3j H H OEt H 51
11 3k Br H OMe H 56
12 3l Br H H OMe 38
13 3m H Br OEt H 51
14 3n H Cl OMe H 54
15 3o H OMe OMe H 59
16 3p H Br OH H 58 c
17 3q H OH OH H 71 c
18 3r H OH OMe H 69 c

a General conditions: reactions were performed with 2 (0.5 mmol), EtMgCl (1.25 equiv.), and azide 1 (1 equiv.) in THF (0.45 M). b Isolated yields of triazoles 3 after flash column chromatography. c Global yield of two steps: formation of the triazole, followed by deprotection of OTBS groups with TBAF.