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Synthesis process of paliperidone palmitate

A technology for paliperidone and a synthesis process, which is applied in the field of synthesis technology of paliperidone palmitate, can solve the problems of waste of resources, low production efficiency, large equipment damage, etc., and achieves low cost, controllable process, and cleanliness of impurities. control effect

Pending Publication Date: 2019-09-20
HUAYU WU XI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The particle size and crystal form of paliperidone palmitate raw material before pulverization have a great influence on the subsequent pulverization. If the particle size of the obtained raw material drug is large and the crystal form is poor, long-term pulverization with a homogenizer and other equipment is required In order to meet the requirements of the preparation, not only the production efficiency is low, waste of resources, but also cause great damage to the equipment

Method used

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  • Synthesis process of paliperidone palmitate
  • Synthesis process of paliperidone palmitate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The synthesis of embodiment 1 paliperidone palmitate

[0037] (1) Synthesis of P:

[0038] a. Add compound A, compound B, DIPA and methanol into the flask, wherein the molar ratio of A:B:DIPA is 1:1:2.1; stir well, use N 2 Protection, start to heat up; reflux reaction for 11h, naturally cool down to 28°C after the reaction to crystallize;

[0039] b. Suction filter the crystal obtained in step a to obtain a filter cake; then the filter cake is beaten and washed with an aqueous solution of methanol with a mass concentration of 45% for 0.5 h; vacuum dried at 50° C. for 7 h to obtain compound P and detected; the yield is about 83.5% .

[0040] (2) Refining of P: feed intake, add the P crude product that step (1) prepares in the flask, then add ethanol and water, wherein the ethanol amount that every 100g P crude product adds is 1.1L by mass volume ratio, the addition of water The volume is 1.4L; in N 2 Heat up under protection until liquid reflux occurs; react until th...

Embodiment 2

[0051] The synthesis of embodiment 2 paliperidone palmitate

[0052] (1) Synthesis of P:

[0053] a. Add compound A, compound B, DIPA and methanol into the flask, wherein the molar ratio of A:B:DIPA is 1:1.2:2.3; stir well, use N 2 Protection, start to heat up; reflux reaction for 13h, naturally cool down to 32°C to crystallize after the reaction is over;

[0054] b. Suction filter the crystal obtained in step a to obtain a filter cake; then the filter cake is beaten and washed with an aqueous solution of methanol with a mass concentration of 55% for 1.5 hours; vacuum dried at 70° C. for 9 hours to obtain compound P and detected; the yield is about 85% .

[0055] (2) Refining of P: feed intake, add the P crude product that step (1) prepares in the flask, then add ethanol and water, wherein the ethanol amount that every 100g P crude product adds is 1.2L by mass volume ratio, the addition of water The volume is 1.6L; in N 2 Heat up under protection until liquid reflux occurs...

Embodiment 3

[0066] The synthesis of embodiment 3 paliperidone palmitate

[0067] (1) Synthesis of P:

[0068] a. Add compound A, compound B, DIPA and methanol into the flask, wherein the molar ratio of A:B:DIPA is 1:1.1:2.2; stir well, use N 2 Protect, start to heat up; reflux reaction for 12 hours, naturally cool down to 30°C after the reaction to crystallize; the yield is about 89.5%;

[0069] b. Suction filter the crystals obtained in step a to obtain a filter cake; then the filter cake is beaten and washed with an aqueous solution of methanol with a mass concentration of 50% for 1 h; vacuum-dried at 60° C. for 8 h to obtain compound P and detected.

[0070] (2) Refining of P: feed intake, add the P crude product that step (1) prepares in the flask, then add ethanol and water, wherein the ethanol amount that every 100g P crude product adds is 1.2L by mass volume ratio, the addition of water The volume is 1.5L; in N 2 Heat up under protection until liquid reflux occurs; react until t...

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Abstract

Belonging to the technical field of pharmaceutical compositions, the invention relates to a synthesis process of paliperidone palmitate. Through synthesis of P (paliperidone), refinement of P synthesis of PP (paliperidone palmitate) and refinement of PP, the paliperidone palmitate can be prepared. According to the invention, the process is controllable, the cost is low, the impurities are controllable, the refining process is simple and convenient, the product purity is high, and the yield is high.

Description

technical field [0001] The invention relates to a synthesis process of paliperidone palmitate, which belongs to the technical field of pharmaceutical compositions. Background technique [0002] Paliperidone palmitate (paliperidone palmitate) is a long-acting injection of the second-generation antipsychotic drug paliperidone, which is mainly used for the treatment of schizophrenia. The active ingredient is paliperidone. The water solubility of paliperidone palmitate is extremely low. During the preparation process, the raw material medicine needs to be crushed into fine particles by homogenizer and other equipment to improve its water solubility, and prepared into a nanocrystal suspension, so as to form a suitable intramuscular injection. The aqueous suspension preparation of the drug increases the absorption rate and bioavailability of the drug. [0003] The particle size and crystal form of paliperidone palmitate raw material before pulverization have a great influence on ...

Claims

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Application Information

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IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 林裕朗
Owner HUAYU WU XI PHARMA
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