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. 2022 Aug 30;87(18):12041–12051. doi: 10.1021/acs.joc.2c01047

Table 1. Study of the Cyclization Reaction of 3a for the Achievement of Piperazinone 4a.

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entry reagents time (h) yield (4a) (%) yield (5a) (%)
1 TFA 50% TES 10% CH2Cl2 40% 4 50 19
2 TFA 50% TIPS 10% CH2Cl2 40% 4 66 17
3 TFA 50% TIPS 40% CH2Cl2 10% 4 70 0
4 TFA 50% TIPS 40% CH2Cl2 10% 16 75 0
5 TFA 50% TIPS 40% 1,2-DCE 10% 16 85 0