反应详情

A mixture of (S)-ethyl 2-(7-(4-(allyloxy)-4-methylpiperidin-1-yl)-2-(azidomethyl)-5-methylpyrazolo[1,5-a]pyrimidin-6-yl)-2-(tert-butoxy)acetate (0.179 g, 0.358 mmol), 3-(allyloxy)-5-methylhex-1-yne (0.109 g, 0.717 mmol), Cu(II)SO4.5H2O (8.95 mg, 0.036 mmol) and (+)-sodium L-ascorbate (0.071 g, 0.358 mmol) in MeOH (2 mL) was stirred for 1 h at rt. Then, purified by prep-HPLC to afford (2S)-ethyl 2-(2-((4-(1-(allyloxy)-3-methylbutyl)-1H-1,2,3-triazol-1-yl)methyl)-7-(4-(allyloxy)-4-methylpiperidin-1-yl)-5-methylpyrazolo[1,5-a]pyrimidin-6-yl)-2-(tert-butoxy)acetate (0.0921 g, 0.141 mmol, 39.4% yield) as pale yellow paste. LCMS (M+H)=652.7.

1. customThen, purified by prep-HPLC