3-Fluoro-4-(methoxycarbonyl)benzeneboronic acid → 3'-Chloro-3-fluoro-4'-[3,3,3-trifluoro-2-(8-fluoro-4-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-2-hydroxy-1-methyl-propyl]-biphenyl-4-carboxylic acid methyl ester

HRID 2096751

反応式

HRID 2096751 の反応式
Br[C:2]1[CH:7]=[CH:6][C:5]([CH:8]([CH3:28])[C:9]([C:15]2[CH:16]=[C:17]([F:27])[C:18]3[O:23][CH2:22][C:21](=[O:24])[N:20]([CH3:25])[C:19]=3[CH:26]=2)([OH:14])[C:10]([F:13])([F:12])[F:11])=[C:4]([Cl:29])[CH:3]=1.[F:30][C:31]1[CH:32]=[C:33](B(O)O)[CH:34]=[CH:35][C:36]=1[C:37]([O:39][CH3:40])=[O:38]>>[CH3:40][O:39][C:37]([C:36]1[CH:35]=[CH:34][C:33]([C:2]2[CH:7]=[CH:6][C:5]([CH:8]([CH3:28])[C:9]([C:15]3[CH:16]=[C:17]([F:27])[C:18]4[O:23][CH2:22][C:21](=[O:24])[N:20]([CH3:25])[C:19]=4[CH:26]=3)([OH:14])[C:10]([F:13])([F:12])[F:11])=[C:4]([Cl:29])[CH:3]=2)=[CH:32][C:31]=1[F:30])=[O:38]

参加物

3

反応物 2

HCID 27828183-Fluoro-4-(methoxycarbonyl)benzeneboronic acidHCID 866458686-[2-(4-bromo-2-chloro-phenyl)-1-hydroxy-1-trifluoromethyl-propyl]-8-fluoro-4-methyl-4H-benzo[1,4]oxazin-3-one

生成物 1

HCID 752403543'-Chloro-3-fluoro-4'-[3,3,3-trifluoro-2-(8-fluoro-4-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-2-hydroxy-1-methyl-propyl]-biphenyl-4-carboxylic acid methyl ester

実験手順

In analogy to Example 17, step 2, 6-[2-(4-bromo-2-chloro-phenyl)-1-hydroxy-1-trifluoromethyl-propyl]-8-fluoro-4-methyl-4H-benzo[1,4]oxazin-3-one was reacted with 3-fluoro-4-methoxycarbonylphenylboronic acid to give the title compound as a colorless foam. MS (m/e)=570.3 [M+H+].

出典と根拠

ORDレコード
ord-0b4c4f5cd6c3456c8971aedf5ba7ec7a
出典データセット
uspto-grants-2013_05
特許番号
US08450313B2

関連ノート

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