4-(3-Fluoro-2-methoxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pentanal → 2-Amino-5-{[4,4-dimethyl-6-fluoro-2-hydroxy-5-methoxy-2-(trifluoromethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]amino}-8-fluoro-quinoline

HRID 1443260노트

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HRID 1443260 반응식
[F:1][C:2]1[C:3]([O:20][CH3:21])=[C:4]([C:8]([CH3:19])([CH3:18])[CH2:9][C:10]([OH:17])([C:13]([F:16])([F:15])[F:14])[CH:11]=O)[CH:5]=[CH:6][CH:7]=1.NC1C=CC(F)=C2C=1C=CC(=O)N2.[NH2:35][C:36]1[CH:45]=[CH:44][C:43]2[C:38](=[C:39]([F:47])[CH:40]=[CH:41][C:42]=2[NH2:46])[N:37]=1>[Ti](Cl)(Cl)(Cl)Cl>[NH2:35][C:36]1[CH:45]=[CH:44][C:43]2[C:38](=[C:39]([F:47])[CH:40]=[CH:41][C:42]=2[NH:46][CH:11]2[C:5]3[C:4](=[C:3]([O:20][CH3:21])[C:2]([F:1])=[CH:7][CH:6]=3)[C:8]([CH3:19])([CH3:18])[CH2:9][C:10]2([OH:17])[C:13]([F:16])([F:14])[F:15])[N:37]=1

참가 물질

5

반응물 3

HCID 179890864-(3-Fluoro-2-methoxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pentanalHCID 179891522,5-Diamino-8-fluoroquinolineHCID 179891895-amino-8-fluoroquinolin-2(1H)-one

생성물 1

HCID 686798322-Amino-5-{[4,4-dimethyl-6-fluoro-2-hydroxy-5-methoxy-2-(trifluoromethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]amino}-8-fluoro-quinoline

시약·촉매·용매 1

HCID 24193Titanium Tetrachloride촉매

실험 절차

Analogously to Example 10, a mixture of the corresponding imines is produced starting from 237 g of 4-(3-fluoro-2-methoxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pentanal and 137 mg of a mixture that consists of 5-amino-8-fluoroquinolin-2(1H)-one and 2,5-diamino-8-fluoroquinoline. Analogously to Example 3, the mixture of imines with 2.5 ml of titanium tetrachloride solution (1 M in dichloromethane) is reacted, and the two title compounds are obtained after chromatography on silica gel.

후처리

  1. customis produced
  2. customis reacted
  3. customthe two title compounds are obtained after chromatography on silica gel

출처 및 근거

ORD 기록
ord-86d770cafe674d60907599032e4d0e79
출처 데이터셋
uspto-grants-2010_02
특허 번호
US07659297B2

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