Water → 7-Fluoro-1,5-naphthyridin-2(1H)-one

HRID 385615노트

반응식

HRID 385615 반응식
[F:1][C:2]1[CH:11]=[C:10]2[C:5]([CH:6]=[CH:7][CH:8]=[N+:9]2[O-])=[N:4][CH:3]=1.C1(C)C=CC(S(Cl)(=O)=[O:20])=CC=1.C(=O)([O-])[O-].[K+].[K+].O>C(Cl)(Cl)Cl>[F:1][C:2]1[CH:11]=[C:10]2[C:5]([CH:6]=[CH:7][C:8](=[O:20])[NH:9]2)=[N:4][CH:3]=1

참가 물질

6

반응물 4

HCID 962WaterHCID 73974-Toluenesulfonyl chlorideHCID 11430Potassium CarbonateHCID 57815215HCID 57815215, 화합물

생성물 1

HCID 469008017-Fluoro-1,5-naphthyridin-2(1H)-one수율 23.3%

시약·촉매·용매 1

HCID 6212Chloroform용매

실험 절차

To a solution of 60 mg of 7-fluoro-1,5-naphthyridine 1-oxide in 1.6 mL of chloroform, 84 mg of p-toluenesulfonyl chloride, 171 mg of potassium carbonate and 0.5 mL of water were added, and the mixture was stirred at room temperature overnight. The solid was filtered off, and purified by silica gel column chromatography using silica gel; Chromatorex-NH made by Fuji Silysia Chemical Ltd., and an eluent of chloroform:methanol=10:1 to obtain 14 mg of 7-fluoro-1,5-naphthyridin-2(1H)-one as a white solid.

후처리

  1. filtrationThe solid was filtered off
  2. custompurified by silica gel column chromatography

출처 및 근거

ORD 기록
ord-5c1595f7189c402b97c6edf44dc6b9d1
출처 데이터셋
uspto-grants-2013_02
특허 번호
US08367831B2

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