Hydrochloric Acid → (R)-(4-fluoro-phenylamino)-phenyl-acetic acid

HRID 77052ノート

反応式

HRID 77052 の反応式
C[O:2][C:3](=[O:19])[C@H:4]([NH:11][C:12]1[CH:17]=[CH:16][C:15]([F:18])=[CH:14][CH:13]=1)[C:5]1[CH:10]=[CH:9][CH:8]=[CH:7][CH:6]=1.Cl>O1CCOCC1>[F:18][C:15]1[CH:16]=[CH:17][C:12]([NH:11][C@H:4]([C:5]2[CH:6]=[CH:7][CH:8]=[CH:9][CH:10]=2)[C:3]([OH:19])=[O:2])=[CH:13][CH:14]=1

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 59401123(R)-(4-fluoro-phenylamino)-phenyl-acetic acid methyl ester

生成物 1

HCID 7006576(R)-(4-fluoro-phenylamino)-phenyl-acetic acid収率 87%

試薬・触媒・溶媒 1

HCID 312751,4-Dioxane溶媒

反応条件

温度
70 °C

実験手順

To a solution of (R)-(4-fluoro-phenylamino)-phenyl-acetic acid methyl ester (I252) (510 mg, 1.97 mmol) in dioxane (10 mL), is added 12N HCl (10 mL) and the mixture is heated at 70° C. for 12 hours. The organic solvent is evaporated, the mixture is cooled to 0° C. and the resulting solid is collected by filtration to obtain intermediate I255 as a brownish solid (420 mg, 87% yield).

後処理

  1. customThe organic solvent is evaporated
  2. temperaturethe mixture is cooled to 0° C.
  3. filtrationthe resulting solid is collected by filtration
  4. customto obtain intermediate

出典と根拠

ORDレコード
ord-ca0cfb9e27b8439b9066a740e8f09515
出典データセット
uspto-grants-2014_09
特許番号
US08835682B2

反応ノート

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