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Alkylol piperazine derivative optical isomer or its salt and its application

A technology of optical isomers and derivatives is applied in the application field of preparing antidepressant drugs, and can solve problems such as large side effects

Inactive Publication Date: 2007-04-18
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] In addition, dual inhibitors that can simultaneously inhibit 5-HT and NA reuptake have the characteristics of good antidepressant effect, small side effects, and rapid onset of action, but triple-action compounds that have inhibitory activity on DA reuptake at the same time have faster onset of action , or showing antidepressant effects while showing relatively large side effects, is still a hot spot in the research of new monoamine antidepressant drugs

Method used

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  • Alkylol piperazine derivative optical isomer or its salt and its application
  • Alkylol piperazine derivative optical isomer or its salt and its application
  • Alkylol piperazine derivative optical isomer or its salt and its application

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Embodiment 1

[0059] Synthesize (1S, 2R)-SIPIyy24 optical isomers by referring to general methods 1-5

[0060] [α] D 25 =-8.05° (C=1, CH 3 OH); mp: 242-243°C (dec); MS: m / z 425 (M+);

[0061] 1 HNMR (DMSO-d6): δ1.05 (d, 3H, NCHCH 3 ), 3.47-4.28 (m, 9H, NCHCH 3 , piperazine-H), 3.99 (s, 3H, OCH 3 ), 5.59 (d, 1H, PhCHOH, J=3.2), 7.45-8.10 (m, 10H, ArH).

[0062] Elemental Analysis: C 25 h 29 ClN 2 o 2 2HCl 2H 2 Theoretical value of O: C: 56.24%, H: 6.51%, N: 5.25%; measured value: C: 56.04%, H: 6.36%, N: 5.30%.

Embodiment 2

[0064] Synthesize (1R, 2S)-SIPIyy24 optical isomers by referring to general methods 1-5

[0065] [α] D 25 =8.54° (C=1, CH 3 OH); mp: 242-243°C (dec); MS: m / z 425 (M+);

[0066] 1 HNMR (DMSO-d6): δ1.05 (d, 3H, NCHCH 3 ), 3.33-4.33 (m, 9H, NCHCH 3 , piperazine-H), 3.99(s, 3H, OCH 3), 5.64 (d, 1H, PhCHOH, J=3.2), 7.45-8.10 (m, 10H, ArH).

[0067] Elemental Analysis: C 25 h 29 ClN 2 o 2 2HCl 2.5H 2 O Theoretical value: C: 55.31%, H: 6.68%, N: 5.16% Measured value: C: 55.20%, H: 6.77%, N: 5.26%

Embodiment 3

[0069] Synthesize (1S, 2S)-SIPIyy24 optical isomers by referring to general methods 1-5

[0070] [α] D 25 =50.60° (C=1, CH 3 OH); mp: 242-243°C (dec); MS: m / z 425 (M+);

[0071] 1 HNMR (DMSO-d6): δ1.07 (d, 3H, NCHCH 3 ), 3.42-3.81 (m, 9H, NCHCH 3 , piperazine-H), 4.41(s, 3H, OCH 3 ), 4.93 (d, 1H, PhCHOH, J=9.6), 7.54-8.21 (m, 10H, ArH).

[0072] Elemental Analysis: C 25 h 29 ClN 2 o 2 2HCl 2H 2 O Theoretical value: C: 56.24%, H: 6.51%, N: 5.25% Measured value: C: 56.44%, H: 6.21%, N: 5.30%

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Abstract

The present invention discloses a alkylolpiperazine derivative optical isomer or its salt, their synthesis method and application. Said invention also provides its chemical structure formula, and said alkylolpiperazine derivative optical isomer can be used fro preparing medicine with the action for resisting depression.

Description

technical field [0001] The present invention relates to a kind of alkanol piperazine derivative optical isomer or its salt, especially relates to N 1 -Benzyl-N 4 -[1-methyl-2-(5'-chloro-6'-methoxy-2'-naphthyl)hydroxyethyl]piperazine or its salt (SIPIyy24 for short, the same below) of the optical isomer Synthesis and its use in the preparation of antidepressant drugs. Background technique [0002] Depression is a common human disease and the most common mental disease that endangers human physical and mental health today. The main symptoms of depression are: depressed mood, decreased activity, changes in appetite or weight, changes in sleep (insomnia or lethargy), fatigue, difficulty concentrating, indecision, and even thoughts of suicide. The incidence of depression in the world is about 3.1%. There are currently about 340 million depressed patients in the world, and about 1 in every 20 people has suffered from depression. In 2005, the incidence of depression will reach ...

Claims

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Application Information

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IPC IPC(8): C07D295/084A61K31/495A61P25/24
CPCC07D295/088A61P25/24
Inventor 李建其翁志洁董文心黄丽瑛金华张绍静顾丰华
Owner SHANGHAI INST OF PHARMA IND
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