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Propellane compounds, preparation method and application thereof

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

Inactive Publication Date: 2011-05-25
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 analgesic effects, but are low in addiction. Therefore, research and development of new opioid analgesics with low addiction is of great clinical significance

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

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Embodiment Construction

[0046] 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.

[0047] 1. Preparation of Compound 2 (X=OMe, R'=Me)

[0048] 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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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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Patent Type & Authority Patents(China)
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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