反应详情

(S)-1-(3-Methoxy-4-nitro-phenyl)-piperidine-3-carboxylic acid was prepared by reacting 4-fluoro-2-methoxy-1-nitro-benzene (342 mg, 2.0 mmol) with (S)-Piperidine-3-carboxylic acid (258 mg, 2.0 mmol) at 80° C. in DMF using K2CO3 (608 mg, 2.20 mmol) as a base scavenger. After 16 h the reaction was concentrated under reduced pressure and the residue was partitioned between EtOAc and water. The aqueous phase was acidified with 1N HCl to pH 4-5. The resulting yellow solid was filtered, rinsed with water, and air dried overnight to yield 352 mg (63%) of (S)-1-(3-Methoxy-4-nitro-phenyl)-piperidine-3-carboxylic acid as a yellow solid. LC/MS (E/I+) 281.08 (M+H).

1. custom(S)-1-(3-Methoxy-4-nitro-phenyl)-piperidine-3-carboxylic acid was prepared
2. customat 80° C.
3. concentrationAfter 16 h the reaction was concentrated under reduced pressure
4. customthe residue was partitioned between EtOAc and water
5. filtrationThe resulting yellow solid was filtered
6. washrinsed with water, and air
7. customdried overnight