Methanesulfonyl chloride → 1-tert-Butyl 2-methyl (2S,4R)-4-((methanesulfonyl)oxy)pyrrolidine-1,2-dicarboxylate

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Reaction Steps

To a solution of methyl (2S,4R)-1-Bochydroxypyrrolidine-2-carboxylate (8 g, 32.65 mmol) prepared in Step B in DCM was added dropwise TEA (11.99 ml, 81.56 mmol) and methanesulfonyl chloride (3.77 ml, 48.9 mmol) at m° C. After the reaction mixture was stirred at rt for 3 h, the organic extracts were washed with a saturated NaHCO3 aqueous solution, 1N HCl and brine, dried over MgSO4, filtered, and concentrated in vacuo to give the title compound (9.4 g, 90%).

Provenance & Evidence