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5-hydroxytryptamine receptor agonist and its preparation method and use

A technology for serotonin and uses, applied in the field of medicinal chemistry, can solve problems such as poor solubility and low stability, and achieve the effects of improving dissolution rate, high stability, and facilitating absorption and utilization

Active Publication Date: 2021-03-26
SICHUAN CREDIT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the crystal forms of the prior art, although the solubility of tandospirone citrate crystal form I is good, its stability is relatively low (see: Chinese patent CN102344442 A); tandospirone citrate Although the stability of ketone crystal form II and crystal form III is relatively high, their solubility is relatively poor (see: Chinese patents CN 103641817 A and CN 103641818 A)

Method used

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  • 5-hydroxytryptamine receptor agonist and its preparation method and use
  • 5-hydroxytryptamine receptor agonist and its preparation method and use
  • 5-hydroxytryptamine receptor agonist and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of Tandospirone Citrate Monohydrate

[0043] Weigh 50g of tandospirone citrate, add 350mL of water, heat up to 100°C, wait until the dissolution is complete, continue stirring for 0.5 hours, then stop heating, stir at 1°C for 1 hour, wait for the solid to precipitate, filter, 50°C After drying under vacuum for 2 hours, 50.3 g of tandospirone citrate monohydrate was obtained, with a yield of 97.5% and a purity of 99.90%. The mass spectrum showed its ESI m / z: 383.

[0044] The measured melting point is: 168.0-169.0°C.

[0045] Get tandospirone citrate monohydrate of the present invention and carry out elemental analysis, the results are shown in Table 1:

[0046] Table 1. Elemental analysis results

[0047] element N％ C％ H％ C 21 h 29 N 5 o 2 ·C 6 h 8 o 7 ·H 2 O theoretical value

11.80 54.63 6.62 The measured value of the product of the present invention 11.80 54.58 6.67

[0048] Determination of l...

Embodiment 2

[0060] Example 2 Preparation of Tandospirone Citrate Monohydrate

[0061] Weigh 50g of tandospirone citrate, add 250mL of water, heat up to 90°C, wait until it is completely dissolved, continue stirring for 0.5 hours, then stop heating, and stir for 6 hours under cooling at 8°C, wait for the solid to precipitate, filter, 40°C Ventilate and dry for 6 hours to obtain 50.5 g of tandospirone citrate monohydrate with a yield of 98.0% and a purity of 99.92%.

[0062] The test results of elemental analysis, loss on drying, moisture determination and thermal analysis of the obtained product show that what the present invention obtains is tandospirone citrate monohydrate.

Embodiment 3

[0063] Example 3 Preparation of Tandospirone Citrate Monohydrate

[0064] Weigh 50g of tandospirone citrate, add 500mL of water, heat up to 50°C, wait until the dissolution is complete, continue stirring for 0.5 hours, then stop heating, stir at 2°C for 4 hours, wait for the solid to precipitate, filter, 15°C After drying under vacuum for 8 hours, 50.4 g of tandospirone citrate monohydrate was obtained, with a yield of 97.8% and a purity of 99.91%.

[0065] The test results of elemental analysis, loss on drying, moisture determination and thermal analysis of the obtained product show that what the present invention obtains is tandospirone citrate monohydrate.

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Abstract

The invention relates to a 5-hydroxytryptamine receptor agonist, a preparing method thereof and uses of the receptor agonist, particularly (3a[alpha],4[beta],7[beta],7a[alpha])-hexahydro-2-[4[4-(2-pyrimidinyl)-1-(piperazinyl)]-butyl]-4,7-methylene-1H-isoindole-1,3(2H)-dione citrate monohydrate, a preparing method thereof and uses of the monohydrate. The molecular formula of the monohydrate is C<21>H<29>N5O2.C6H8O<7>.H2O. The monohydrate has advantages of high stability and good solubility, thus facilitating product quality control, increasing dissolution rates of preparations, and facilitating medicine absorption and utilization. The monohydrate can be prepared into various dosage forms conveniently, and is convenient to process, store and convey. The preparing method has advantages of few steps, simple and convenient operation, a high product yield, high purity, and the like and is particularly suitable for industrial application.

Description

technical field [0001] The invention relates to tandospirone citrate monohydrate and its preparation method and application. belongs to the field of medicinal chemistry. Background technique [0002] Tandospirone, the chemical name is (3aα,4β,7β,7aα)-hexahydro-2-[4[4-(2-pyrimidinyl)-1-(piperazinyl)-butyl]-4,7 -Methylene-1H-isoindole-1,3(2H)-dione, whose structural formula is as follows; Tandospirone is a serotonin receptor agonist, mainly used in the treatment of anxiety or other states accompanied by anxiety disease. [0003] [0004] Tandospirone belongs to the azaspirone class of drugs. In the brain, it can interact with 5-HT in the hippocampus, septum, interpeduncular nucleus, amygdala and other brain limbic systems concentrated in the emotional center and suture gland nucleus. 1A Receptors selectively bind by agonizing 5-HT 1A Autoreceptors, regulate the 5-HT projected from the raphe nucleus to the hippocampus, inhibit the 5-HT effect of the action inhibition sys...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/12A61K31/506A61P25/22A61P25/24A61P25/00A61P25/20A61P25/18A61P25/28A61P3/04A61P15/10A61P25/30A61P25/32A61P25/16A61P25/08A61P13/00A61P27/06A61P27/02A61P29/00A61P25/02A61P9/14
CPCC07B2200/13C07D403/12
Inventor 陈刚李晓莉刘志鸿傅霖邓丽敏
Owner SICHUAN CREDIT PHARMA
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