Hydrochloric Acid → Tert-butyl 3-(1-aminoethyl)azetidine-1-carboxylate

Participants

Reaction Conditions

Reaction Steps

To a solution 3-[1-(2-methyl-propane-2-sulfinylamino)-ethyl]-azetidine-1-carboxylic acid tert-butyl ester (crude from step 2, 264 mg, 0.87 mmol) in MeOH at 0° C. was added 4.0 M HCl in dioxane (0.28 mL, 1.13 mmol) dropwise. The reaction mixture was stirred at 0° C. for 1 h then quenched with saturated aqueous NaHCO3, diluted with water and extracted with CH2Cl2 (3×). The combined organics were dried over MgSO4 and concentrated to afford 3-(1-amino-ethyl)-azetidine-1-carboxylic acid tert-butyl ester as a thick colorless oil which was used without further purification.

Provenance & Evidence