Toluene → 2-(4-(4-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)butanoyl)phenyl)-2-methylpropanoic acid

HRID 227597ノート

反応式

HRID 227597 の反応式
Cl[CH2:2][CH2:3][CH2:4][C:5]([C:7]1[CH:12]=[CH:11][C:10]([C:13]([CH3:18])([CH3:17])[C:14]([OH:16])=[O:15])=[CH:9][CH:8]=1)=[O:6].[N:19]1(CO)[CH2:24][CH2:23][CH2:22][CH2:21][CH2:20]1.[C:27]([O-:30])([O-])=O.[K+].[K+].[C:33]1(C)[CH:38]=[CH:37][CH:36]=[CH:35][CH:34]=1>>[OH:30][C:27]([C:33]1[CH:34]=[CH:35][CH:36]=[CH:37][CH:38]=1)([C:7]1[CH:12]=[CH:11][CH:10]=[CH:9][CH:8]=1)[CH:22]1[CH2:21][CH2:20][N:19]([CH2:2][CH2:3][CH2:4][C:5]([C:7]2[CH:12]=[CH:11][C:10]([C:13]([CH3:18])([CH3:17])[C:14]([OH:16])=[O:15])=[CH:9][CH:8]=2)=[O:6])[CH2:24][CH2:23]1

参加物

5

反応物 4

HCID 1140TolueneHCID 11430Potassium CarbonateHCID 446909Piperidin-1-ylmethanolHCID 109235672-(4-(4-Chlorobutanoyl)phenyl)-2-methylpropanoic acid

生成物 1

HCID 99356992-(4-(4-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)butanoyl)phenyl)-2-methylpropanoic acid

実験手順

A mixture of 800 mg of 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid, prepared in accordance with Example 4, 800 mg of 4-α,α-diphenyl)piperidinemethanol, and 2.4 g of K2CO3 in 25 mL of toluene is stirred for 48 hours at room temperature. The mixture is concentrated in vacuo. The residue is treated with EtOAc, filtered, and concentrated to afford 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetic acid.

後処理

  1. concentrationThe mixture is concentrated in vacuo
  2. additionThe residue is treated with EtOAc
  3. filtrationfiltered
  4. concentrationconcentrated

出典と根拠

ORDレコード
ord-4b1c7d2bdf53448db2d485e81f802f5e
出典データセット
uspto-grants-2009_07
特許番号
US07560561B2

反応ノート

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