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Processes for preparation of ziprasidone

A technology of ziprasidone and reaction, which is applied in the field of preparation of ziprasidone, and can solve problems such as yield decline and no further reaction

Inactive Publication Date: 2007-01-17
TEVA PHARMA IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The difference in the levels of remaining CEI and BITP is problematic because if CEI is depleted, remaining BITP is no longer responsive
The remaining BITP becomes an impurity and leads to a decrease in yield

Method used

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  • Processes for preparation of ziprasidone
  • Processes for preparation of ziprasidone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0080] 1 Preparation of ZPR with 0.9 mol NaI in n-BuOH.

[0081] Add n-BuOH (50 ml) and 1,2-benzisothiazole-3-piperazinyl hydrochloride (BITP HCl) (5.6 g, 0.022 mol) into a three-necked flask, and heat the resulting slurry at 100°C. At 110°C, Na was added to the slurry 2 CO 3 (11.6g), NaI (3g) and 5-(2-chloroethyl)-6-chloro-1,3-dihydro-indol-2(2H)-one (CEI) (7.5g, 0.032mol) . Heating was continued for 8.5 hours. After the reaction was cooled, the product was filtered, washed with hexane and water, and dried at 60°C. The dried product weighed 8.12 g and had a HPLC purity of 92.7%.

[0082] 2. Preparation of ZPR in Glycerol

[0083] Add BITP HCl (25g, 0.098mol), glycerol (62ml), Na 2 CO 3 (13 g), the mixture was stirred for 10 minutes. CEI (5.9 g) was added to the reaction mixture, and the reaction mixture was heated at 115-120° C. for 3 hours. After 3 hours, the reaction was nearly complete; after cooling to room temperature, the solid was filtered off, triturated in ...

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Abstract

Provided are processes for preparing ziprasidone from 1, 2-benzothiazole-3-piperazinyl (BITP) and 5-(2-chloroethyl)-6-chloro-1, 3-dihydro-indole-2(2H) one (CEI) using various solvents, bases and promoters.

Description

[0001] related application [0002] This application claims the benefit of US Provisional Applications Serial No. 60 / 514,096, filed October 24, 2003, and US Provisional Application Serial No. 60 / 515,328, filed October 28, 2003, both of which are incorporated herein in their entirety. field of invention [0003] The invention relates to a preparation method of ziprasidone. Background of the invention [0004] Ziprasidone is an antipsychotic that is chemically unrelated to phenothiazine or butyrophenone antipsychotics. The chemical name of ziprasidone is as follows: 5-[2-[4-1,2-Benzisothiazol-3-yl]-1-piperazinyl]ethyl]-6-chloro-1,3-di Hydrogen-2H-indol-2-one, the structure is: [0005] [0006] Ziprasidone is administered to a host such as a mammal, preferably a human, for the treatment of psychiatric disorders such as schizophrenia. Other uses of ziprasidone are disclosed in WO 03 / 070246, WO 01 / 91756, incorporated here...

Claims

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Application Information

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IPC IPC(8): C07D417/12
Inventor G·皮拉斯基N·申卡M·门德洛维奇T·尼达姆A·巴拉诺夫
Owner TEVA PHARMA IND LTD
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