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A 5-hydroxytryptamine receptor agonist, a preparing method thereof and uses of the receptor agonist

A serotonin and solid technology, applied in the field of medicinal chemistry, can solve the problems of poor solubility and low stability, and achieve the effects of easy operation, high stability, superior formability and

Active Publication Date: 2017-02-15
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 high, their solubility is relatively poor (see: Chinese patents CN 103641817 A and CN 103641818 A)

Method used

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  • A 5-hydroxytryptamine receptor agonist, a preparing method thereof and uses of the receptor agonist
  • A 5-hydroxytryptamine receptor agonist, a preparing method thereof and uses of the receptor agonist
  • A 5-hydroxytryptamine receptor agonist, a preparing method thereof and uses of the receptor agonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Weigh 20g of tandospirone citrate, add 140mL of water, heat up to 70°C, wait for complete dissolution, cool down to 40±5°C, add 100mL of acetone and 100mL of diethyl ether under stirring, continue to cool down to room temperature and stir for 1 hour, 5 Stir at ±5°C for 1 hour, wait for the solid to precipitate, filter, and vacuum dry at 50°C for 2 hours to obtain 19.6 g of tandospirone citrate 4 / 5 hydrate with a yield of 95.6% and a purity of 99.93%.

[0038] Mass spectrum showed its ESI m / z: 383.

[0039] Get product of the present invention to carry out elemental analysis, the results are shown in Table 1.

[0040] Table 1. Elemental analysis results

[0041] element N％ C％ H％ C 21 h 29 N 5 o 2 · C 6 h 8 o 7 · 4 / 5H 2 O theoretical value

11.87 54.96 6.59 The measured value of the product of the present invention 11.88 54.94 6.58

[0042] Determination of loss on drying: the product of the present invention was dri...

Embodiment 2

[0049] Weigh 20g of tandospirone citrate, add 300mL of water, heat up to 50°C, wait for complete dissolution, cool down to 40±5°C, add 150mL of acetone and 250mL of diethyl ether under stirring, continue to cool down to room temperature and stir for 3 hours, 5 Stir at ±5°C for 1 hour, wait for the solid to precipitate, filter, and vacuum dry at 35°C for 8 hours to obtain 19.8 g of tandospirone citrate 4 / 5 hydrate with a yield of 96.6% and a purity of 99.90%.

[0050] 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 4 / 5 hydrate.

Embodiment 3

[0052] Weigh 20g of tandospirone citrate, add 100mL of water, heat up to 90°C, wait for complete dissolution, cool down to 40±5°C, add 40mL of acetone and 60mL of ether under stirring, continue to cool down to room temperature and stir for 15 minutes, 5 Stir at ±5°C for 4 hours, wait for solid precipitation, filter, and vacuum dry at 15°C for 10 hours to obtain 19.5 g of tandospirone citrate 4 / 5 hydrate with a yield of 95.1% and a purity of 99.93%.

[0053] 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 4 / 5 hydrate.

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PUM

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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 4 / 5-hydrate, a preparing method thereof and uses of the 4 / 5-hydrate. The molecular formula of the 4 / 5-hydrate is C<21>H<29>N5O2.C6H8O<7>.(4 / 5)H2O. The 4 / 5-hydrate has advantages of high stability and good solubility, and therefore product quality control is facilitated and the 4 / 5-hydrate can be prepared into various dosage forms conveniently. The 4 / 5-hydrate has excellent compactibility and tabletting performance so that the 4 / 5-hydrate can be easily processed into tablets and is convenient to 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 4 / 5 hydrate, a preparation method and application thereof. 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12C07C59/265C07C51/41C07C51/43A61K31/506A61P25/00A61P27/02A61P25/18A61P25/20A61P25/22A61P25/24A61P3/04A61P25/30A61P25/32A61P15/00A61P15/10A61P25/08A61P25/16A61P27/06A61P3/10A61P25/04
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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