tert-Butyl (2R)-2-{4-[(4-chlorophenyl)methyl]-4H-1,2,4-triazol-3-yl}pyrrolidine-1-carboxylate → 4-[(4-Chlorophenyl)methyl]-3-[(2R)-pyrrolidin-2-yl]-4H-1,2,4-triazole

Participants

Reaction Steps

De-Boc by HCl procedure: A solution of Boc-protected triazole from Example 3 (1.95 g, 5.374 mmol) in 100 mL of 4 N HCl in dioxane was stirred at room temperature for 4 h. The mixture was concentrated in vacuo and then treated with minimum amount of MeOH, diluted with ether, white crystal precipitated out. After filtration, the white crystal was collected and dried in vacuo to yield the HCl salt of desired product (1.67 g, 92.6%, yield calculated based on 2 eq. HCl attached).

Provenance & Evidence