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. 2014 Aug 20;16(17):4504–4507. doi: 10.1021/ol502048e

Table 1. Optimization for the Synthesis of 4 and 5.

graphic file with name ol-2014-02048e_0008.jpg

entry solvent t (°C) time/h (4a/5a) yield (%)a
1 MeOH rt 24 33/41
2 EtOH rt 24 62/19
3 DMF rt 24 trace/trace
4 DCE rt 24 57/13
5 CH3CN rt 24 48/23
6 toluene rt 24 72/<5
7 THF rt 24 62/10
8 1,4-dioxane rt 24 74/<5
9 MeOH 60 1 39/34
10 1,4-dioxane 60 1 68/<5
a

Isolated yield.

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