Diisopropylethylamine → Rac-n-((3s,4r)-1-benzyl-4-o-tolyl-pyrrolidin-3-yl)-2-(3,5-dichloro-phenyl)-n-methyl-isobutyramide

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Reaction Steps

A solution of 2-(3,5-dichloro-phenyl)-2-methyl-propionyl chloride (the preparation of which is described in WO2005002577) (127 mg, 0.50 mmol) in CH2Cl2 (5 ml) was added drop wise to a stirred solution of ((3S,4R)-1-benzyl-4-o-tolyl-pyrrolidin-3-yl)-methyl-amine (the preparation of which is described herein above) (135 mg, 0.48 mmol) and ethyl-diisopropyl-amine (0.12 ml, 0.72 mmol) in CH2Cl2 (5 ml). The reaction mixture was stirred 2 h, concentrated under vacuo and purification by flash chromatography (SiO2, EtOAc/H, 1:3) yielded 0.18 g (75%) of the title product as colorless oil.

Provenance & Evidence