Bromoacetyl bromide → 5-chloro-thiophene-2-carboxylic acid [(R)-1-(2-bromo-acetyl)-pyrrolidin-3-yl]-amide

Participants

Reaction Steps

7.1 A solution of 400 mg 5-chloro-thiophene-2-carboxylic acid (R)-pyrrolidin-3-ylamide hydrochloride (example 6.2) in 5 ml THF was treated with 0.31 ml TEA and 0.16 ml bromo acetylbromide. The reaction mixture was stirred over night. The precipitate was filtered and washed with THF. The filtrate was concentrated. The crude product was purified by chromatography (silica gel; gradient: CH2Cl2 to CH2Cl2/MeOH 98:2) to give 250 mg 5-chloro-thiophene-2-carboxylic acid [(R)-1-(2-bromo-acetyl)-pyrrolidin-3-yl]-amide. Off-white amorphous solid. 353.1 ([M+H]+)

Provenance & Evidence