Toluene → 2-(4-Bromo-2-fluorophenyl)pyrimidine

HRID 1038104ノート

反応式

HRID 1038104 の反応式
[Br:1][C:2]1[CH:7]=[CH:6][C:5](B(O)O)=[C:4]([F:11])[CH:3]=1.Br[C:13]1[N:18]=[CH:17][CH:16]=[CH:15][N:14]=1.C(=O)([O-])[O-].[Na+].[Na+].C1(C)C=CC=CC=1>C(O)C>[Br:1][C:2]1[CH:7]=[CH:6][C:5]([C:13]2[N:18]=[CH:17][CH:16]=[CH:15][N:14]=2)=[C:4]([F:11])[CH:3]=1

参加物

6

反応物 4

HCID 1140TolueneHCID 10340Sodium CarbonateHCID 783452-BromopyrimidineHCID 27733334-Bromo-2-fluorobenzeneboronic acid

生成物 1

HCID 576857022-(4-Bromo-2-fluorophenyl)pyrimidine

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

実験手順

4-Bromo-2-fluorophenyl boronic acid (2AB) (3.0 g, 13.71 mmol, 1 equiv), 2-bromopyrimidine (1AB) (6.54 g, 41.13 mmol, 3 equiv), and 2M sodium carbonate (34 mL) were added in a pressure vessel (350 mL) and a (1v:1v) mixture of toluene and ethanol (45 mL: 45 mL) was added. The mixture was then bubbled with nitrogen gas for about 10 minutes. Tetrakistriphenylphosphine palladium (0) (793 mg, 0.686 mmol, 0.05 equiv) was added to the mixture. The reaction vessel was tightly capped, placed in an oil bath at 90° C. and stirred overnight.

後処理

  1. additionwas added
  2. customThe mixture was then bubbled with nitrogen gas for about 10 minutes
  3. customThe reaction vessel was tightly capped
  4. customplaced in an oil bath at 90° C.

出典と根拠

ORDレコード
ord-6c43dc03f62748e6911c519a5e2b221e
出典データセット
uspto-grants-2013_10
特許番号
US08546404B2

反応ノート

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