Dimethylformamide → (2S)-1-(Benzyloxycarbonyl)azetidine-2-carboxylic acid chloride

Participants

Reaction Conditions

Reaction Steps

(2S)-1-(benzyloxycarbonyl)azetidine-2-carboxylic acid (729.3 mg, 3.10 mmol, 1.0 eq) was dissolved in dry dichloromethane (15 mL) and cooled to about −5° C. under argon. Oxalyl chloride (380 μL, 4.36 mmol, 1.4 eq) and a drop of DMF were added to the solution. The mixture was warmed to reflux temperature with stirring over about a 3 hour period. After cooling, the mixture was concentrated and used in Reference Example 16.

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