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. Author manuscript; available in PMC: 2011 Nov 5.
Published in final edited form as: Org Lett. 2010 Nov 5;12(21):4936–4939. doi: 10.1021/ol1022036

Table 2.

One-pot, three-step synthesis of 1,4-disubstituted triazoles 3

graphic file with name nihms-245231-t0004.jpg

entry Ar-X R method Aa
yield (%)
method Bb
yield (%)

1 Ph-I Bn 96 91
2 4-MeO-C6H4-I Bn 41 54
3 4-CF3-C6H4-I Bn 97 98
4 4-F-C6H4-I Bn 98 98
5 4-Me-C6H4-I Bn 93 95
6 2-Me-C6H4-I Bn 97 98
7 Ph-Br Bn 42 65
8 4-MeO-C6H4-Br Bn 13 15(57c)
9 4-NO2-C6H4-Br Bn 12 11(53c)
10 Ph-I 4-MeO-Bn\ 84 91
11 Ph-I 4-NO2-Bn 97 98
a

A mixture of TBAF (1.0 M, 2.0 equiv) and CuI (10 mol %) was used

b

CuF2 (2.0 equiv) was used

c

The Sonogashira cross coupling was performed using Pd(PPh3)2Cl2 (5 mol %), CuI (10 mol %) in refluxing Et3N for 10 h.