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A technology of lurasidone hydrochloride and hydrochloric acid is applied in the preparation field of lurasidone hydrochloride, which can solve the problems of low acetone and the like, and achieve the effects of improving durability, high yield, and improving stability and reliability.
Inactive Publication Date: 2012-10-24
SHANGHAI INST OF PHARMA IND +1
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[0007] The technical problem to be solved by the present invention is to overcome the defect of lurasidone hydrochloride with low acetone residue, high purity and high yield in the preparation method of existing lurasidone hydrochloride, which needs harsher conditions, And a kind of preparation method of lurasidone hydrochloride with high durability is provided
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Embodiment 1
[0025] (3aR, 4S, 7R, 7aS)-2-[(1R, 2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexyl Methyl]hexahydro-1H-4,7-methylisoindole 1,3-dione (Compound II) (5 g) was dissolved in acetone (53 g) with heating. Under reflux state, dropwise add the acetone (12g) solution of 36% hydrochloric acid (1.13g), reflux and stir for 2h after dropwise addition, after cooling to room temperature, filter, obtain lurasidone hydrochloride (5.16g) after vacuum drying at 60°C. g, yield 96%): HPLC purity 99.86%, the largest single impurity 0.06%, acetone residue 0.13%.
Embodiment 2
[0027] (3aR, 4S, 7R, 7aS)-2-[(1R, 2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexyl Methyl]hexahydro-1H-4,7-methylisoindole 1,3-dione (compound II) (2 g) was heated and dissolved in acetone (21.2 g). Under reflux state, dropwise add the acetone (6.5g) solution of 18% hydrochloric acid (0.91g), reflux and stir 2h after dropwise addition, after cooling to room temperature, filter, obtain lurasidone hydrochloride ( 2.14 g, yield 99%): HPLC purity 99.83%, the maximum simplex 0.06%, acetone residue 0.21%.
Embodiment 3
[0029] (3aR, 4S, 7R, 7aS)-2-[(1R, 2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexyl Methyl]hexahydro-1H-4,7-methylisoindole 1,3-dione (compound II) (2 g) was heated and dissolved in acetone (21.2 g). Under reflux, add 14.4% hydrochloric acid (1.13g) in acetone (6.5g) dropwise. After the dropwise addition, stir at the same temperature for 2 hours. After cooling to room temperature, filter, and vacuum dry at 60°C to obtain lurazil hydrochloride Ketone (1.95 g, yield 95%): HPLC purity 99.83%, maximum simplex 0.07%, residual acetone 0.051%.
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Abstract
The present invention discloses a preparation method for lurasidone hydrochloride represented by a formula (I). The method comprises the following steps: adopting a mixture to treat a solution formed by dissolving a compound (II) in a dialkyl ketone solvent having carbon number not more than 6, and carrying out crystallization to obtain the product of the present invention, wherein the mixture comprise an organic solvent capable of mixing and dissolving with water and hydrochloric acid, a mass ratio of the organic solvent to the hydrochloric acid is 0.5:1-100:1, a molar ratio of hydrogen chloride in the hydrochloric acid to the compound II is 10:1-0.9:1. The preparation method of the present invention has the following advantages that: durability is significantly improved, the prepared lurasidone hydrochloride (the compound I) has characteristics of high purity, low residual acetone, and high yield, and the method is economical and is suitable for industrial production.
Description
technical field [0001] The present invention specifically relates to a preparation method of lurasidone hydrochloride. Background technique [0002] Lurasidone hydrochloride (lurasidone hydrochloride), also known as lurasidone hydrochloride, can be used for the treatment of mental diseases (such as schizophrenia). Its chemical structure is shown in structural formula I. [0003] [0004] According to the report of patent document JP-A-5-17440 and its family of patents EP0464846, the above-mentioned compound I can be obtained by processing the acetone solution of its free base (compound II) with an isopropanol solution of hydrogen chloride, but the above-mentioned method is not suitable for large-scale industrialization Production. [0005] [0006] According to the report of Chinese patent 200480022168.7, the acetone solution of compound II needs to be treated with 1.8% to 5.0% hydrochloric acid to obtain lurasidone hydrochloride (compound I) with low acetone residue...
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