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Aralkylone pipeazine derivative and its application

一种芳烷酮哌嗪、衍生物的技术，应用在芳烷酮哌嗪衍生物领域，能够解决胃蠕动减少等问题

Inactive Publication Date: 2002-11-27
NHWA PHARMA CORPORATION +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] One of the technical problems to be solved in the present invention is to disclose a class of aralkylone piperazine compounds with medical value, to overcome the defects of existing drugs with side effects such as addiction, respiratory depression, and gastric motility reduction, and to solve clinical problems. Meet people's analgesic needs;

Method used

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  • Aralkylone pipeazine derivative and its application
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1IV-1

[0098] Example 1IV-1 N 1 -Benzyl-N 4 -Phenylmethylpiperazine hydrochloride

[0099] N-benzylpiperazine hydrochloride 3.98g (16mmol), acetophenone chloride 2.97g (19.2mmol) and anhydrous K 2 CO 3 7.73g (56mmol) was synthesized in acetone according to general method two to obtain 4.5g of white solid, yield 75%, mp 238-9°C.

[0100] Elemental analysis: C 19 H 22 N 2 O·2HCl·H 2 O (theoretical value%: C 59.31, H 6.8, N 7.27, Cl 18.4; experimental value% C 59.38, H 6.51, N 7.12, Cl 18.23)

[0101] IR(KCl): ν2950, ​​1710, 1600, 1500cm -1 .

[0102] 1 HNMR(DMSO-d 6 ): δ3.58 (m, 8H, piperazine-H), 4.50 (s, 2H, PhCH 2 ), 5.22(s, 2H, COCH 2 N), 7.40-8.10 (m, 10H, ArH).

[0103] MS: m / z 294(M + )

Embodiment 2IV-2

[0104] Example 2IV-2 N 1 -P-chlorobenzyl-N 4 -(1-Benzoylethyl)piperazine hydrochloride

[0105] Take N-p-chlorobenzylpiperazine hydrochloride 5g (20mmol), anhydrous KHCO 3 (70mmol) and 3.96ml (26mmol) of 2-bromopropiophenone, reacted at reflux in 40ml of absolute ethanol for 8 hours. After treatment according to the general method, the product is 6.1g, yield 59.51%, mp260-262℃

[0106] Elemental analysis: C 20 H 23 ClN 2 O·2HCl·H 2 O (theoretical value%: C 55.37, H 6.27, N 6.46; experimental value% C55.01, H 6.01, N 6.41)

Embodiment 3IV-3

[0107] MS: m / z 342(M + ) Example 3IV-3 N 1 -P-chlorobenzyl-N 4 -Phenylmethylpiperazine hydrochloride

[0108] Take 5g (20mmol) of N-p-chlorobenzylpiperazine hydrochloride, 5.58ml (40mmol) of triethylamine and 4.08g (26mmol) of chloroacetophenone, reflux for 8 hours in 40ml of absolute ethanol, press the pass After the second treatment method, the product is 5.2g, the yield is 59.51%, mp256-258℃

[0109] Elemental analysis: C 19 H 21 ClN 2 O·2HCl·H 2 O (theoretical value%: C 55.37, H 6.27, N 6.46; experimental value% C55.01, H 6.01, N 6.41)

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Abstract

An aralkylone piperazine derivative and its application to preparing antalgic and sedative medicines are disclosed. Its advantages are high antalgic effect to control nerve, no dependency, low poisonand little nerve by-effect.

Description

Technical field [0001] The invention relates to an aralkanone piperazine derivative and its application as a novel analgesic and tranquilizer. Background technique [0002] Severe acute and chronic pain, including tumor pain and postoperative pain, plagues tens of millions of patients, and is currently a major clinical problem. Due to the addictive nature of the existing opioid analgesics, respiratory depression, reduced gastric motility and other side effects, which limit their widespread use, we are looking for a center that can maintain a strong analgesic effect, but also overcome the above-mentioned drawbacks, and be safe for clinical use. Analgesic drugs are not only the main research goal in the field of analgesia, but also an important area of ​​innovative drug research. Summary of the invention [0003] One of the technical problems that the present invention needs to solve is to disclose a class of aralkanone piperazine compounds with medical value, so as to overcome th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61P25/24C07D295/108
CPCA61K31/495C07D295/108A61P25/24
Inventor 李建其黄丽瑛张椿年唐希灿胡国渊
Owner NHWA PHARMA CORPORATION
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