2-Fluoro-4-(methoxycarbonyl)benzeneboronic acid → 4-[5-Chloro-2-(2-fluoro-4-methoxycarbonyl-phenyl)-pyridin-4-ylethynyl]-piperidine-1-carboxylic acid tert-butyl ester

HRID 1184711ノート

反応式

HRID 1184711 の反応式
[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][CH:11]([C:14]#[C:15][C:16]2[C:21]([Cl:22])=[CH:20][N:19]=[C:18](Cl)[CH:17]=2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[F:24][C:25]1[CH:30]=[C:29]([C:31]([O:33][CH3:34])=[O:32])[CH:28]=[CH:27][C:26]=1B(O)O>>[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][CH:11]([C:14]#[C:15][C:16]2[C:21]([Cl:22])=[CH:20][N:19]=[C:18]([C:26]3[CH:27]=[CH:28][C:29]([C:31]([O:33][CH3:34])=[O:32])=[CH:30][C:25]=3[F:24])[CH:17]=2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2]

参加物

3

反応物 2

HCID 248243452-Fluoro-4-(methoxycarbonyl)benzeneboronic acidHCID 866748934-(2,5-Dichloro-pyridin-4-ylethynyl)-piperidine-1-carboxylic acid tert-butyl ester

生成物 1

HCID 679737414-[5-Chloro-2-(2-fluoro-4-methoxycarbonyl-phenyl)-pyridin-4-ylethynyl]-piperidine-1-carboxylic acid tert-butyl ester

実験手順

The title compound is prepared from 4-(2,5-dichloro-pyridin-4-ylethynyl)-piperidine-1-carboxylic acid tert-butyl ester and 2-fluoro-4-methoxycarbonyl-phenylboronic acid following a procedure analogous to that described for Intermediate 14. LC (method 7): tR=1.76 min; Mass spectrum (ESI+): m/z=473 [M+H]+.

出典と根拠

ORDレコード
ord-6ed20b080b14402298bc69e1bfa9c7d4
出典データセット
uspto-grants-2014_03
特許番号
US08669271B2

反応ノート

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