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Preparation method of crystal a of lurasidone hydrochloride

A technology of lurasidone hydrochloride and hydrochloride, applied in the field of preparation of crystal A, can solve problems such as the problem that crystal form is not described, and achieve the effect of safe and high-purity production and preparation process

Inactive Publication Date: 2016-06-22
SHANDONG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] JP2003160583A, JP2006169154, JP2006169155 and WO200509999 all report the synthesis method of lurasidone and its hydrochloride, but they do not describe the problem of crystal form

Method used

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  • Preparation method of crystal a of lurasidone hydrochloride
  • Preparation method of crystal a of lurasidone hydrochloride
  • Preparation method of crystal a of lurasidone hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Add 13.7 g of crude lurasidone hydrochloride to 206 ml of DMF, heat to 100°C to dissolve completely, cool to room temperature under stirring (30 rpm), and filter after 2 hours. Dry at 60°C to obtain lurasidone hydrochloride crystal A9.5g. HPLC purity reaches 99.75% (see Figure 4 ), the melting point measured by DSC was 271.8°C.

Embodiment 2

[0042] Add 2.3 g of crude bulurasidone hydrochloride to 4.6 ml of DMF, heat to 100° C., then cool to room temperature while stirring (50 rpm), and filter after 2 hours. Dry at 60°C. Obtained lurasidone hydrochloride crystal A2.1g.

Embodiment 3

[0044] Add 5 g of crude lurasidone hydrochloride to 125 ml of DMF, heat to 30° C., then cool to room temperature while stirring (800 rpm), and filter after 2 hours. Dry at 60°C. Obtained lurasidone hydrochloride crystal A3.4g.

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Abstract

The invention discloses a lurasidone HCl crystal A preparing method. Lurasidone HCl is mixed with organic alcohol, and crystallization is carried out on the condition of stirring. The organic alcohol is one or more of carbinol, ethanol and isopropanol. The invention further discloses another lurasidone HCl crystal A preparing method. The Lurasidone HCl is mixed with N,N-dimethylformamide, and crystallization is carried out on the condition of stirring. The invention further provides a lurasidone HCl crystal A preparing method. The Lurasidone HCl is mixed with carbinol and then dissolving is carried out, and a crystal is separated by standing. The crystal A is a single crystal. The volume mass ratios of the carbinol and the lurasidone HCl are 50-200 mL / g. According to the methods, the lurasidone HCl crystal A with good water-solubility can be obtained, the methods are simple, productivity is high, wide industrial prospect is achieved, and residual toxic solvent amount is low.

Description

technical field [0001] The invention relates to a preparation method of crystal A of lurasidone hydrochloride. Background technique [0002] The polymorphic form of a drug is one of the factors that affect the quality of the drug. It has a non-negligible impact on the preparation of raw materials and pharmaceutical preparations, as well as the stability, dissolution rate and bioavailability of the preparations, and some even bring toxic side effects. , so it is of great significance to study the crystal form of drugs. [0003] (3aR, 4S, 7R, 7aS)-2-{(1R, 2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-yl]methyl of the following structural formula ]Cyclohexylmethyl}hexahydro-4,7-methylene-2H-isoindole-1,3-dione hydrochloride is commonly called lurasidone hydrochloride (lurasidoneHCl), and its CAS number is 367514-88-3, jointly developed by Japan's Sumitomo and Daiichi Sankyo Pharmaceutical, was approved by the FDA in October 2010 for marketing in the United States, as a 5-HT2A...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D417/12
Inventor 隋强翟雪刘帅王小梅时惠麟
Owner SHANDONG UNIV