Trimethyl borate → [4-(Difluoromethyl)phenyl]boronic acid

反応式

[F:1][CH:2]([F:10])[C:3]1[CH:8]=[CH:7][C:6](I)=[CH:5][CH:4]=1.C([Mg]Cl)(C)C.[B:16](OC)([O:19]C)[O:17]C>>[F:1][CH:2]([F:10])[C:3]1[CH:8]=[CH:7][C:6]([B:16]([OH:19])[OH:17])=[CH:5][CH:4]=1

参加物

反応物 3

HCID 8470Trimethyl borate

HCID 463117371-(Difluoromethyl)-4-iodobenzene

HCID 178418918HCID 178418918、化合物

生成物 1

HCID 20777176[4-(Difluoromethyl)phenyl]boronic acid

実験手順

In a departure from the procedure described above the compound is prepared from 4-difluoromethyl-1-iodo-benzene (prepared from 4-iodobenzaldehyde using diethylaminosulfurtrifluoride (DAST) in dichloromethane) using iPrMgCl to generate the arylmetal compound and trapping this intermediate with trimethyl borate.

出典と根拠

ORDレコード: ord-578649c648b84fa593df4981d55ea478
出典データセット: uspto-grants-2010_08
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07776830B2

反応ノート

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