Water → Ethyl 1-(2,4-dimethoxybenzyl)-7-(2-hydroxymethylpiperidin-1-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylate

HRID 1867937노트

반응식

HRID 1867937 반응식
Cl[C:2]1[N:11]=[C:10]2[C:5]([C:6](=[O:28])[C:7]([C:23]([O:25][CH2:26][CH3:27])=[O:24])=[CH:8][N:9]2[CH2:12][C:13]2[CH:18]=[CH:17][C:16]([O:19][CH3:20])=[CH:15][C:14]=2[O:21][CH3:22])=[CH:4][C:3]=1F.N1([CH2:36][OH:37])CCCCC1.[CH:38](N(C(C)C)CC)([CH3:40])[CH3:39].O.[C:48](#[N:50])[CH3:49]>>[CH3:22][O:21][C:14]1[CH:15]=[C:16]([O:19][CH3:20])[CH:17]=[CH:18][C:13]=1[CH2:12][N:9]1[C:10]2[C:5](=[CH:4][CH:3]=[C:2]([N:50]3[CH2:40][CH2:38][CH2:39][CH2:49][CH:48]3[CH2:36][OH:37])[N:11]=2)[C:6](=[O:28])[C:7]([C:23]([O:25][CH2:26][CH3:27])=[O:24])=[CH:8]1

참가 물질

6

반응물 5

HCID 962WaterHCID 6342AcetonitrileHCID 81531DiisopropylethylamineHCID 446909Piperidin-1-ylmethanolHCID 13937202Ethyl 7-chloro-1-(2,4-dimethoxybenzyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylate

생성물 1

HCID 69030307Ethyl 1-(2,4-dimethoxybenzyl)-7-(2-hydroxymethylpiperidin-1-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylate

반응 조건

온도
75 °C

실험 절차

A mixture of EXAMPLE 1B (2.15 g), piperidinylmethanol (890 mg) and diisopropylethylamine (2.5 mL) in acetonitrile (50 mL) at 25° C. was stirred for 24 hours, heated at 75° C. for 5 days, cooled, treated with water, and extracted with dichloromethane (200 mL). The extract was washed with water and 1M hydrochloric acid and concentrated.

후처리

  1. temperaturecooled
  2. extractionextracted with dichloromethane (200 mL)
  3. washThe extract was washed with water and 1M hydrochloric acid
  4. concentrationconcentrated

출처 및 근거

ORD 기록
ord-be7ac9be88d94205aa7e39f7e88acfe6
출처 데이터셋
uspto-grants-2009_12
특허 번호
US07632946B2

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