Triethylamine → 7-[4-(2-Hydroxyethylidene)piperidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid

HRID 15504노트

반응식

HRID 15504 반응식
C([N:3]([CH2:6][CH3:7])[CH2:4][CH3:5])C.Cl[C:9]1[N:18]=[C:17]2[C:12]([C:13](=[O:25])[C:14]([C:22]([OH:24])=[O:23])=[CH:15][N:16]2[CH:19]2[CH2:21][CH2:20]2)=[CH:11][C:10]=1[F:26]>C(#N)C>[OH:23][CH2:22][CH:14]=[C:13]1[CH2:5][CH2:4][N:3]([C:9]2[N:18]=[C:17]3[C:12]([C:13](=[O:25])[C:14]([C:22]([OH:24])=[O:23])=[CH:15][N:16]3[CH:19]3[CH2:21][CH2:20]3)=[CH:11][C:10]=2[F:26])[CH2:6][CH2:7]1

참가 물질

4

반응물 2

HCID 8471TriethylamineHCID 110551427-Chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid

생성물 1

HCID 593424447-[4-(2-Hydroxyethylidene)piperidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid수율 79.2%

시약·촉매·용매 1

HCID 6342Acetonitrile용매

실험 절차

A solution of amine 103 (256 mg, 1.06 mmol) and triethylamine (0.5 mL, 3.55 mmol) in acetonitrile (4 mL) was treated with 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-naphthyridine-3-carboxylic acid (200 mg, 0.71 mmol) under nitrogen and the reaction mixture was allowed to stir for 16 h. The resulting mixture was concentrated in vacuo, and the residue was washed with water (3×10 mL) and allowed to dry overnight to afford the title compound 163 (105 mg, 40%). MS 374 (M+H).

후처리

  1. concentrationThe resulting mixture was concentrated in vacuo
  2. washthe residue was washed with water (3×10 mL)
  3. customto dry overnight

출처 및 근거

ORD 기록
ord-d6cbd9c94be14219b07239531cfb199d
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07732612B2

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