Ethyl chloroacetate → N-[(3S)-1-[6-chloro-5-[[(cyclohexylmethyl)amino]carbonyl]-2-quinolinyl]-3-pyrrolidinyl]-glycine, Ethyl Ester

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A stirred solution of 2-[(3S)-3-Amino-1-pyrrolidinyl]-6-chloro-N-(cyclohexylmethyl)-5-quinolinecarboxamide (prepared as in Example 44) (450 mg), ethyl chloroacetate (0.21 mL) and triethylamine (0.33 mL) in acetonitrile (3 mL) was heated at 100° C. in a microwave for 1 hour after which it was cooled to room temperature and concentrated. Purification by chromatography (SiO2, dichloromethane:methanol:ammonia in methanol (7 M) 96:3:1 as eluant) gave the subtitle compound as a solid (490 mg).

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