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 1443260ノート

反応式

HRID 1443260 の反応式
[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

参加物

5

反応物 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

生成物 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

試薬・触媒・溶媒 1

HCID 24193Titanium Tetrachloride触媒

実験手順

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.

後処理

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

出典と根拠

ORDレコード
ord-86d770cafe674d60907599032e4d0e79
出典データセット
uspto-grants-2010_02
特許番号
US07659297B2

反応ノート

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