Piconol → (RS)-[2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-ethoxy-acetic acid ethyl ester

反応式

[CH2:1]([O:3][C:4](=[O:18])[CH:5]([C:9]1[C:14]([F:15])=[CH:13][C:12]([OH:16])=[CH:11][C:10]=1[F:17])[O:6][CH2:7][CH3:8])[CH3:2].O[CH2:20][C:21]1[CH:26]=[CH:25][CH:24]=[CH:23][N:22]=1>>[CH2:1]([O:3][C:4](=[O:18])[CH:5]([C:9]1[C:14]([F:15])=[CH:13][C:12]([O:16][CH2:20][C:21]2[CH:26]=[CH:25][CH:24]=[CH:23][N:22]=2)=[CH:11][C:10]=1[F:17])[O:6][CH2:7][CH3:8])[CH3:2]

参加物

反応物 2

HCID 11474Piconol

HCID 69290842(RS)-(2,6-difluoro-4-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester

生成物 1

HCID 69291981(RS)-[2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-ethoxy-acetic acid ethyl ester

実験手順

In analogy to example 22.1 (RS)-(2,6-difluoro-4-hydroxy-phenyl)-ethoxy-acetic acid ethyl ester (example L6) was reacted with 2-(hydroxymethyl)pyridine to give (RS)-[2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-ethoxy-acetic acid ethyl ester as a yellow semisolid. This material was hydrolysed in analogy to example 101.3 to give (RS)-[2,6-difluoro-4-(pyridin-2-ylmethoxy)-phenyl]-ethoxy-acetic acid. White solid. MS 324.1 ([M+H]+)

出典と根拠

ORDレコード: ord-70d51dc71daf486a8a74d8f32a479546
出典データセット: uspto-grants-2006_10
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07129238B2

反応ノート

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