Chloroacetyl chloride → HCID 66564636, compound

Participants

Reaction Steps

3-Aminomethyl-piperidine-1-carboxylic acid tert-butyl ester 1c (5.0 g, 23.4 mmol) in 20 mL CH2Cl2 was added dropwise to a cold (−10→0° C.) solution of chloroacetylchloride (2.8 mL, 35 mmol, 1.5 equiv) and diisopropylethylamine (6.1 mL, 35 mmol, 1.5 equiv) in 60 mL CH2Cl2 under N2. After being left overnight (−10° C.→rt), the mixture was diluted with ethyl acetate and washed briefly with water and brine, dried (Na2SO4), and concentrated to give 3-[(2-chloroacetylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester 1d as a dark brown oil. The crude product was used without further purification.

Provenance & Evidence