Triethylamine → Tert-butyl 4-(2-fluorobenzoyl)piperazine-1-carboxylate

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Reaction Steps

To a solution of piperazine-1-carboxylic acid tert-butyl ester (10 g, 53.7 mmol) in dichloromethane (300 mL), add triethyl amine (15.1 mL, 107.4 mmol) and 2-fluorobenzoyl chloride (6.4 mL, 53.7 mmol). Stir the mixture at room temperature overnight. Then add water (200 mL) and separate the organic layer, dry over sodium sulfate, filter and evaporate solvent under reduced pressure to give 17.3 g of 4-(2-fluoro-benzoyl)-piperazine-1-carboxylic acid tert-butyl ester. ES+ (m/z) 309[M+H].

Provenance & Evidence