(3S)-(-)-3-Aminopyrrolidine → 2-[(3S)-3-Amino-1-pyrrolidinyl]-6-chloro-N-(cyclohexylmethyl)-5-quinolinecarboxamide

Participants

Reaction Conditions

Reaction Steps

A stirred suspension of 2,6-dichloro-N-(cyclohexylmethyl)quinoline-5-carboxamide (Example 43(a)) (500 mg) and (3S)-3-pyrrolidinamine (0.60 mL) in acetonitrile (3 mL) was heated at 100° C. in a microwave for 40 minutes after which it was cooled to room temperature and concentrated. Purification by chromatography (SiO2, dichloromethane:methanol:ammonia in methanol (7 M) 95:5:0.5 as eluant) and subsequent recrystallisation (acetonitrile) afforded the title compound as a solid (280 mg).

Provenance & Evidence