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Method for preparing lurasidone

A technology of lurasidone and its compound, which is applied in the field of preparation of lurasidone, can solve the problems of incomplete reaction, high preparation cost, and long reaction time, and achieve the effects of low cost, high yield, and easy operation

Inactive Publication Date: 2013-02-06
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The technical problem to be solved by the present invention is to overcome the defects of long reaction time, incomplete reaction, high preparation cost, complicated post-treatment process and unsuitability for industrial large-scale preparation in the existing preparation method of lurasidone. And a kind of preparation method of lurasidone is provided

Method used

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  • Method for preparing lurasidone
  • Method for preparing lurasidone
  • Method for preparing lurasidone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Preparation of Compound I

[0026]

[0027] 5g (11.8mmol) of compound II, 2.2g (13.3mmol) of compound IV and 1.9g (13.7mmol) of potassium carbonate were placed in a reaction flask, and 100ml of N,N-dimethylformamide (DMF) was added, heated to 130 °C, react for 4 hours. After the reaction, 100ml of water was added, stirred at room temperature for 2 hours, a large amount of solid was precipitated, filtered, and the filter cake was washed with water to obtain a white solid, which weighed 5.25g after drying, with a yield of 90%.

[0028] Its structural identification data are as follows:

[0029] 1 H NMR (DMSO-d 6 )δ: ppm 1.1-1.2 (3H, d), 2.0-2.1 (2H, m), 2.5-2.6 (1H, dd), 2.8-2.9 (2H, t), 2.96-3.0 (1H, dd), 3.3 -3.5(3H, m), 3.5-3.7(4H, m), 4.2-4.3(2H, t), 4.3-4.4(2H, t), 4.6-4.7(2H, m), 4.8-5.2(1H, br), 6.9-7.15 (6H, m), 7.3-7.4 (2H, m), 8.0-8.1 (2H, m).

Embodiment 2

[0030] Example 2 Preparation of Compound I

[0031]

[0032] Put 5g of compound II, 2.2g of compound IV and 1.9g of potassium carbonate in a reaction flask, add 100ml of N,N-dimethylformamide (DMF), heat to 50°C, and react for 24 hours. After the reaction was finished, add 100ml of water, stir at room temperature for 2 hours, a large amount of solids were separated out, filtered, and the filter cake was washed with water to obtain a white solid, which weighed 3.4g after drying, and the yield was 60%. The structural identification data was the same as in Example 1.

Embodiment 3

[0033] Example 3 Preparation of Compound I

[0034]

[0035] Put 5g of compound II, 2.2g of compound IV and 1.9g of potassium carbonate in a reaction flask, add 100ml of N,N-dimethylformamide (DMF), heat to 150°C, and react for 3 hours. After the reaction was finished, add 100ml of water, stir at room temperature for 2 hours, a large amount of solids were separated out, filtered, and the filter cake was washed with water to obtain a white solid, which weighed 5.0g after drying, with a yield of 86%, and its structural identification data was the same as in Example 1.

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Abstract

The invention discloses a method for preparing lurasidone as shown in format I. The method comprises the following steps: in a polar aprotic solvent, under the action of alkali, a compound II or a compound III and a compound IV are reacted as follows at the temperature of 50-150 DEG C. The method for preparing lurasidone has the advantages of high yield, simplicity and convenience in operation and low cost and is suitable for industrial mass production. A new way is provided for the preparation of lurasidone.

Description

technical field [0001] The invention relates to a preparation method of lurasidone. Background technique [0002] Mental illness is a common disease, affecting about one percent of the population. With the accelerated pace of life and frequent social interactions, mental illness has increasingly become a frequent disease, especially in cities with a relatively concentrated population. At present, antipsychotic drugs have annual sales of 16.2 billion US dollars in the global market, making them the fifth largest therapeutic category after cholesterol-lowering drugs. [0003] Among the existing antipsychotic drugs, haloperidol, olanzapine and other drugs are likely to cause weight gain, and the extrapyramidal adverse reactions are serious; ziprasidone mesylate is effective in controlling the acute agitation symptoms of schizophrenia, and There were no adverse reactions of weight gain, but there were adverse reactions of cardiac QT prolongation. [0004] Lurasidone hydrochlo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12
Inventor 隋强翟雪王小梅时惠麟
Owner SHANGHAI INST OF PHARMA IND CO LTD
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