Process for the preparation of polymorphs of selective serotonin reuptake inhibitor

A technology of crystal form and solvent is applied in the field of preparation of selective serotonin reuptake inhibitor polymorph, and can solve the problems of undisclosed solid state properties of sertraline hydrochloride and the like

Inactive Publication Date: 2007-01-24
CIPLA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But this patent does not disclose the solid-state proper

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  • Process for the preparation of polymorphs of selective serotonin reuptake inhibitor

Examples

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Embodiment 1

[0040] Preparation of Sertraline Hydrochloride Form II

[0041] 20 grams of sertraline acetate was suspended in a mixture of 100 ml of isopropanol and 4 ml of toluene. The mixture was heated to 50°C to obtain a clear solution, and dried hydrogen chloride gas was introduced to adjust the pH to 1-2. The reaction exothermed and the temperature rose to 60°C. The reaction was gradually cooled to room temperature. The precipitated solid was filtered and washed with isopropanol, and dried in a vacuum at 80° C. for 4 to 5 hours to obtain Sertraline Hydrochloride Form II.

Embodiment 2

[0043] Preparation of Sertraline Hydrochloride Form III

[0044] 20 grams of sertraline acetate was suspended in a mixture of 100 ml of isopropanol and 4 ml of toluene. The mixture was heated to 50°C to obtain a clear solution, and dried hydrogen chloride gas was passed through to adjust the pH to 1-2. The reaction exothermed and the temperature rose to 60°C. The reaction mixture was quickly cooled to 15-20°C in an ice bath within 15-20 minutes. The precipitated solid was filtered, washed with isopropanol, and dried in vacuum at 80° C. for 4 to 5 hours to obtain Sertraline Hydrochloride Form III.

Embodiment 3

[0046] Preparation of Sertraline Hydrochloride Form IV

[0047] Suspend 50 grams of sertraline acetate in 250 ml of isopropanol at room temperature. The mixture was heated to 50°C to obtain a clear solution, and dried hydrogen chloride gas was passed in to adjust the pH to 1-2. The reaction mixture was cooled to 15-20°C within 30 minutes with stirring. The precipitated solid is filtered and washed with isopropanol, and dried in a fluidized bed dryer at 60° C. for 4 to 5 hours to obtain Sertraline Hydrochloride Form IV.

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Abstract

The present invention relates to sertraline hydrochloride crystal forms II, III, IV and V and a preparation method thereof. According to the present invention, various polymorphs of sertraline hydrochloride can be prepared directly from sertraline base or from sertraline acetate.

Description

Technical field [0001] The invention relates to a method for preparing various polymorphs of sertraline hydrochloride from sertraline base or sertraline acetate. The method is rugged and is suitable for mass production of various crystal forms of sertraline hydrochloride, that is, crystal forms II, III, IV and V. Background technique [0002] Sertraline hydrochloride with formula 1, (1S-cis)-4-(3,4 dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthylamine hydrochloride It is approved by the U.S. Food and Drug Administration for the treatment of depression, obsessive-compulsive disorder and panic disorder, with the trade name Zoloft(R). [0003] [0004] Formula 1 [0005] U.S. Patent No. 4,536,518 ("the '518 Patent") describes the preparation of sertraline hydrochloride with a melting point of 243-245°C by treating an ethyl acetate / ether solution of free base with hydrogen chloride gas. However, the patent does not disclose the solid-state prope...

Claims

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Application Information

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IPC IPC(8): C07C209/84C07C211/42A61K31/135
CPCC07C209/84A61P25/22A61P25/24A61P43/00C07C211/42
Inventor 德哈马拉杰·拉马钱德拉·拉奥拉金德拉·纳拉扬拉奥·坎坎
Owner CIPLA LTD
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