Propellane compounds, preparation method and application thereof

A compound, propane technology, applied in the field of propane compounds, can solve the problems of low addiction and limited application, etc.

Inactive Publication Date: 2009-04-08
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the tolerance and dependent side effects of this type of drug, its application is greatly limited.
κ-opioid receptor agonists also have powerful

Method used

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  • Propellane compounds, preparation method and application thereof
  • Propellane compounds, preparation method and application thereof
  • Propellane compounds, preparation method and application thereof

Examples

Experimental program
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Embodiment Construction

[0045] 1 HNMR was measured with a Varian Mercury AMX300 instrument; MS was measured with a VGZAB-HS or VG-700 instrument, and all were EI sources (70ev) unless otherwise specified; all solvents used were re-distilled or anhydrous before use; all All the reactions were carried out under the protection of argon, and the progress of the reaction was tracked by TLC. Post-treatments were washed with saturated brine and dried over anhydrous sodium sulfate; unless otherwise specified, silica gel (200-300 mesh) column chromatography was used for product purification; silica gel and silica gel plates used included 200-300 mesh silica gel and GF254 silica gel plate. Both are products of Qingdao Ocean Chemical Factory or Yantai Yuanbo Silicone Co., Ltd.

[0046] 1. Preparation of Compound 2 (X=OMe, R'=Me)

[0047] Compound 3 (X=OMe, R'=Me) (5.67g, 18.0mmol) was dissolved in 100mL of mixed acid of acetic acid and concentrated hydrochloric acid, refluxed at 120°C, and zinc powder (17.7g...

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PUM

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Abstract

The invention discloses propellane compounds, a preparation method and application thereof, in particular aromatic or fat thick heterocyclic propellane compounds, a preparation method thereof and applications for treating drug abuse as an opioid receptor excitant or an antagonist and for using as a novel analgesic agent and so on. The structures of the compounds are shown in a general formula (I).

Description

technical field [0001] The present invention relates to a class of propeller alkanes and its preparation method, as opioid receptor agonist or antagonist, to treat drug abuse and brain dysfunction related to drug abuse, and as a new type of analgesic. Background technique [0002] Drug abuse is a serious social and economic problem that directly endangers human health and destroys family unity. It is a chronic disease of the brain caused by long-term excessive use of excitatory substances such as cocaine and heroin. It is characterized by a slow course of disease and high relapse, accompanied by obvious psychological, intellectual and behavioral disorders [Crome, HB. Drug Alcohol Depend. 1999, 55: 247-263; NIDA (2000): Epidemiologic Trends in Drug Abuse, NIH Publication No. 00-4739A. National Institute on Drug Abuse, 99]. In recent years, with the development of neurobiology, neuropharmacology, molecular biology, molecular genetics, brain imaging technology, etc., human be...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07D221/18A61K31/437A61P25/04A61P25/00
Inventor 张翱谢欣李付营
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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