Hydrochloric Acid → 3-Fluoro-4-methoxyphenylboronic acid

HRID 36821

反応式

HRID 36821 の反応式
[Mg].Br[C:3]1[CH:8]=[CH:7][C:6]([O:9][CH3:10])=[C:5]([F:11])[CH:4]=1.[B:12](OC(C)C)([O:17]C(C)C)[O:13]C(C)C.Cl>C1COCC1>[CH3:10][O:9][C:6]1[CH:7]=[CH:8][C:3]([B:12]([OH:17])[OH:13])=[CH:4][C:5]=1[F:11]

参加物

6

実験手順

Then, 9.6 g of magnesium was added to 230 ml of THF, and the solution thus formed was slowly added dropwise with 70.9 g of the 4-bromo-2-fluoroanisole obtained by the procedure mentioned above to prepare a Grignard reagent. The reagent was added dropwise to a mixture of 123.8 g of triisopropyl borate and 391 ml of THF at a temperature of -60° C. to -50° C. with stirring. After the dropping of the reagent was finished, the solution was subjected to reaction at an ambient temperature for 2 hours, added with 242 ml of a 1N-aqueous hydrochloric acid solution, subjected to further reaction for 1 hour, extracted with an ether, washed with water, and concentrated under a reduced pressure to obtain 46.2 g of 4-methoxy-3-fluorobenzene boronic acid.

後処理

  1. customthe solution thus formed
  2. customobtained by the procedure
  3. customthe solution was subjected to reaction at an ambient temperature for 2 hours
  4. customsubjected to further reaction for 1 hour
  5. extractionextracted with an ether
  6. washwashed with water
  7. concentrationconcentrated under a reduced pressure

出典と根拠

ORDレコード
ord-25b0f0e5e9c241c398e5745d30c58bb2
出典データセット
uspto-grants-1995_05
特許番号
US05417885

関連ノート

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