Methanol → 3-Pyrrolidinecarbonitrile, 4-(2,4-difluorophenyl)-, (4R)-

Participants

Reaction Conditions

Reaction Steps

To a solution of (4R)-1-t-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonitrile (4 g, 15.15 mmol) prepared according to the procedure described in WO 2004/09126 in DCE (10 ml) was added dropwise 1-chloroethyl chloroformate (2.45 ml, 22.68 mmol) at 0° C. The reaction solution was heated to 70° C., and maintaining this temperature, 1.8-bis(dimethylamino)naphthalene (4.87 g, 22.72 mmol) in DCE (10 ml) was added dropwise for 2 h. After the reaction finished, methanol (10 ml) was added, and maintaining the temperature, the reaction mixture was stirred for additional 1 h, concentrated in vacuo, and the next reaction was carried out without further purification.

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