反応式
[CH:1]1[CH:2]=[CH:3][C:4]([CH:7]([N:15]2[CH2:20][CH2:19][N:18]([CH2:21][CH2:22][O:23][CH2:24][C:25]([OH:27])=[O:26])[CH2:17][CH2:16]2)[C:8]2[CH:9]=[CH:10][C:11]([Cl:14])=[CH:12][CH:13]=2)=[CH:5][CH:6]=1.C1(C(N2CCN(CCO)CC2)C2C=CC([Cl:41])=CC=2)C=CC=CC=1.[K].CC([O-])(C)C.[K+].[Cl:58]CC([O-])=O.[Na+]>>[CH:1]1[CH:2]=[CH:3][C:4]([CH:7]([N:15]2[CH2:20][CH2:19][N:18]([CH2:21][CH2:22][O:23][CH2:24][C:25]([OH:27])=[O:26])[CH2:17][CH2:16]2)[C:8]2[CH:9]=[CH:10][C:11]([Cl:14])=[CH:12][CH:13]=2)=[CH:5][CH:6]=1.[ClH:41].[ClH:58]参加物
実験手順
The process of UK-P No. 2 225 320 (Chem. Abstr., 113, 191395s) aims at the elimination of the disadvantages of the above known processes by preparing cetirizine from the {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol of the formula III which is converted to the potassium salt with potassium tert-butylate. The potassium salt is reacted with sodium chloro-acetate to obtain cetirizine dihydrochloride in a yield of 48.8%. In addition, 5.1% of a second generation product are obtained. Also an improved process is described for the preparation of the {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol of the formula III according to which 1-[(4-chlorophenyl)phenyl-methyl]piperazine of the formula VI is reacted with ethylene chlorohydrine in a yield of 90.4%, the total yield of the synthesis, referred to the piperazine derivative of the formula VI, is merely 48.7%.
出典と根拠
- ORDレコード
- ord-a63f0f0fe1ef487fa2253d6c3dd5f958
- 出典データセット
- uspto-grants-2005_06
- 特許番号
- US06908999B2
関連ノート
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