Dimethylformamide → 1-{[1-(4-Chlorophenyl)cyclopropyl]carbonyl}pyrrolidin-3-ol

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Reaction Steps

3-Pyrrolidinol (1.81 g, 0.0208 mol) was added to a mixture of 1-(4-chlorophenyl)cyclopropanecarboxylic acid (3.93 g, 0.0200 mol), benzotriazol-1-yloxytris(dimethylamino) phosphonium hexafluorophosphate (8.84 g, 0.0200 mol) and 4-methylmorpholine (9.00 mL, 0.0819 mol) in N,N-dimethylformamide (20.0 mL, 0.258 mol). The mixture was stirred at rt overnight. The mixture was diluted with ethyl acetate (100 mL) and was washed with NaHCO3 (7.5%, 3×30 mL). The organic layer was dried over Na2SO4, filtered and concentrated under reduced pressure. The residue was used directly in the next step without further purification.

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