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. 2012 Nov 8;8:1901–1908. doi: 10.3762/bjoc.8.220

Table 1.

Optimization of the reaction conditions for conversion of substrate 2a to 9a.

Entry Brønsted acid Solvent Temp (oC) Time (h) Producta

1 1% TFA DCM rt 24 0
2 1% triflic acid DMF rt 24 0
3 p-TsOH Toluene 120 24 0
4 AcOH Ethanol 100 24 0
5 2% MSA ACN 80 24 0
6 2% MSA DMF 120 16 0
7 2% triflic acid ACN 80 24 27
8 2% triflic acid DMF 120 16 87
9 5% triflic acid DMF 120 16 80
10 1% triflic acid DMF 120 16 75
11 0.5% triflic acid DMF 120 16 35

abased on HPLC.