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Preparation method of tartaric acid pimavanserin crystal form A

A technology of pimavanserin and tartaric acid, which is applied in the field of preparation of pimavanserin tartrate crystal form A, can solve the problem of low yield and crystal form purity of crystal form C, low crystal form purity, and crystal form A between batches big differences etc.

Pending Publication Date: 2021-06-08
NKD PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the preparation of crystal form A has become a key step in the preparation of pimavanserin tartrate, but the crystal form A prepared by the prior art has large differences between batches, and its crystal form has low purity and contains other unknown crystal forms, making the preparation The obtained crystal form C yield and crystal form purity are lower

Method used

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  • Preparation method of tartaric acid pimavanserin crystal form A
  • Preparation method of tartaric acid pimavanserin crystal form A
  • Preparation method of tartaric acid pimavanserin crystal form A

Examples

Experimental program
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Effect test

Embodiment 198

[0069] Embodiment 1 prepares pimavanserin tartrate crystal form A with 98% ethanol aqueous solution

[0070] Salt formation: Add 9.94kg of pimavanserin and 98% ethanol aqueous solution (49.71kg) into the reaction kettle, stir and heat up to 50°C, and drop L-tartaric acid (1.74kg)-98 % ethanol aqueous solution (8.70kg), after adding, cool down to 40°C and stir for 0.5h. After a large amount of solids are precipitated, cool down to -5°C, and crystallize at -5°C for 2h, centrifuge and dry, and the wet product is directly refined .

[0071] Refining: add the above-mentioned pimavanserin tartrate filter cake and 98% ethanol aqueous solution (49.71kg) to 2 reaction kettles, stir and raise the temperature to 75°C, cool down to 45°C for crystallization for 0.5h after the material liquid dissolves, a large amount of solid After precipitation, cool down to 15°C, control the temperature at 15°C for crystallization for 2 hours, centrifuge, rinse with 98% ethanol aqueous solution, spin dr...

Embodiment 298

[0074] Example 2 Preparation of pimavanserin tartrate crystal form A with 98.5% aqueous ethanol

[0075] Salt formation: Add 9.94kg of pimavanserin and 98.5% ethanol aqueous solution (49.71kg) into the reaction kettle, stir and heat up to 40°C, and drop L-tartaric acid (1.74kg)-98.5 % ethanol aqueous solution (13.92kg), after adding, cool down to 40°C and stir for 0.5h. After a large amount of solids are precipitated, cool down to 0°C, and crystallize at 0°C for 2h, centrifuge to dry, and the wet product is directly refined.

[0076] Refining: add the above-mentioned pimavanserin tartrate filter cake and 98.5% ethanol aqueous solution (49.71kg) to 2 reaction kettles, stir and heat up to 78°C, cool down to 45°C to crystallize for 0.5h after the material solution dissolves, a large amount of solid After precipitation, cool down to 20°C, control the temperature at 20°C for crystallization for 2 hours, centrifuge, rinse with 98.5% ethanol aqueous solution, spin dry, and dry in vac...

Embodiment 395

[0079] Embodiment 3 prepares pimavanserin tartrate crystal form A with 95% ethanol aqueous solution

[0080] Salt formation: Add 9.94kg of pimavanserin and 95% ethanol aqueous solution (49.71kg) into the reaction kettle, stir and heat up to 50°C, and drop L-tartaric acid (1.74kg)-95 % ethanol aqueous solution (5.22kg), after adding, cool down to 45°C and stir for 0.5h. After a large amount of solids are precipitated, cool down to 5°C, and crystallize at 5°C for 2h, centrifuge to dry, and the wet product is directly refined.

[0081] Refining: add the above-mentioned pimavanserin tartrate filter cake and 95% ethanol aqueous solution (49.71kg) to 2 reaction kettles, stir and heat up to 75°C, cool down to 45°C for 0.5h to crystallize after the material liquid dissolves, a large amount of solid After the precipitation, cool down to 15°C, control the temperature at 15°C for crystallization for 2 hours, centrifuge, rinse with 95% ethanol aqueous solution, spin dry, and dry in a vacu...

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Abstract

The invention relates to the fields of medicines and chemistry, in particular to a preparation method of a tartaric acid pimavanserin crystal form A. The method comprises the following steps: dissolving a compound shown as a formula (I) in a solvent; cooling the obtained solution; separating to obtain a precipitated solid, wherein the solvent is an ethanol aqueous solution with the concentration of 90.0 to 98.5 percent, an isopropanol aqueous solution with the concentration of 90.0 to 98.5 percent, or a mixed aqueous solution of ethanol and isopropanol with the concentration of 90.0 to 98.5 percent. According to the method, the high-purity tartaric acid pimavanserin crystal form A can be stably prepared.

Description

technical field [0001] The application relates to the fields of medicine and chemistry, in particular to a preparation method of pimavanserin tartrate crystal form A. Background technique [0002] Pimavanserin tartrate was developed by ACADIA and was approved by the U.S. Food and Drug Administration (FDA) in April 2016. The product name is first to market It is a film-coated oral tablet with a specification of 17mg / tablet, which has been withdrawn from the market at present. In June 2018, the new dosage form of pimavanserin tartrate capsules was re-approved by the FDA, with a specification of 34mg / capsule. The main indication of the drug is Parkinson's disease complicated mental illness, the market size is huge, and the industry is very optimistic about its commercial prospects. [0003] At present, the optimal preparation route of pimavanserin is as follows: [0004] [0005] Pimavanserin is salted with tartaric acid in a solvent to prepare pimavanserin tartrate. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/58C07C51/43C07C59/255G01N23/207G01N25/04
CPCC07D211/58C07C51/43G01N23/207G01N25/04C07B2200/13
Inventor 高宏伟马建佳黄志勇高启福方泉
Owner NKD PHARMA CO LTD
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