Sodium Iodide → Ziprasidone

HRID 1925221

反応式

HRID 1925221 の反応式
[CH:1]1[CH:2]=[CH:3][C:4]2[S:9][N:8]=[C:7]([N:10]3[CH2:15][CH2:14][N:13]([CH2:16][CH2:17][C:18]4[CH:19]=[C:20]5[CH2:28][C:26](=[O:27])[NH:25][C:21]5=[CH:22][C:23]=4[Cl:24])[CH2:12][CH2:11]3)[C:5]=2[CH:6]=1.Cl.S1C2C=CC=CC=2C(N2CCNCC2)=N1.ClCCC1C=C2C(=CC=1Cl)NC(=O)C2.[I-].[Na+].C(=O)([O-])[O-].[Na+].[Na+]>C(C(C)=O)C(C)C>[CH:1]1[CH:2]=[CH:3][C:4]2[S:9][N:8]=[C:7]([N:10]3[CH2:11][CH2:12][N:13]([CH2:16][CH2:17][C:18]4[CH:19]=[C:20]5[CH2:28][C:26](=[O:27])[NH:25][C:21]5=[CH:22][C:23]=4[Cl:24])[CH2:14][CH2:15]3)[C:5]=2[CH:6]=1

参加物

7

反応物 5

HCID 5238Sodium IodideHCID 10340Sodium CarbonateHCID 219099Ziprasidone HydrochlorideHCID 27721443-(1-Piperazinyl)-1,2-benzisothiazoleHCID 106094745-(2-Chloroethyl)-6-chlorooxindole

生成物 1

HCID 60854Ziprasidone

試薬・触媒・溶媒 1

HCID 7909Methyl Isobutyl Ketone溶媒

実験手順

U.S. Pat. No. 4,831,031 discloses a process for the preparation of ziprasidone hydrochloride, which involves refluxing N-(1,2-benzisothiazol-3-yl)piperazine with 5-(2-chloroethyl)-6-chloro-oxindole in methyl isobutyl ketone in the presence of sodium iodide and sodium carbonate for about 40 hours followed by column chromatographic purification of the product to get ziprasidone base which is dissolved in methylene chloride and treated with ethereal hydrogen chloride to get ziprasidone hydrochloride salt. The salt is washed with acetone and the product is dried.

後処理

  1. customfollowed by column chromatographic purification of the product

出典と根拠

ORDレコード
ord-a1fe5bcacab64580aac065d315eeeb4c
出典データセット
uspto-grants-2012_05
特許番号
US08178674B2

関連ノート

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