Pyridine → Benzyl-(2S)-2-aminocarbonyl4,4-difluoropyrrolidine-1-carboxylate

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Reaction Steps

To a stirred solution of 1-[(benzyloxy)carbonyl]4,4-difluoro-L-proline, pyridine (0.6 eq.) and di-t-butyl dicarbonate (1.3 eq) in dioxane, ammonium bicarbonate (1.26 eq) was added and the mixture was stirred at room temperature for 20 hours. Dioxane was concentrated and the residue dissolved in ethyl acetate and washed with HCl 1 N, saturated aqueous NaHCO3 and brine, dried over Na2SO4, filtered and evaporated in vacuo to obtain a yellow oil.

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