Hydrochloric Acid → (R)-4-[3-((S)-4-Hydroxy-6-aza-spiro[2.5]oct-6-yl)-propyl]-2-methyl-[1,4]diazepan-5-one dihydrochloride

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Reaction Steps

A solution of 0.500 g (1.26 mmol) of (R)-4-[3-((S)-4-hydroxy-6-aza-spiro[2.5]oct-6-yl)-propyl]-2-methyl-5-oxo-[1,4]diazepane-1-carboxylic acid tert-butyl ester (example ID) in 8 ml of dichloromethane was treated at 0° C. with 3.16 ml (12.64 mmol, 10 eq.) of 4 M hydrogen chloride solution in dioxane. The solution was stirred overnight and warmed up to room temperature. The solution was evaporated, suspended in toluene and evaporated (3 times) to give 0.610 g (quantitative, purity: 76%) of the title compound as white solid. MS: 296.3 (MH+).

Provenance & Evidence