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Heterocycle-fused morphinans compounds, preparation method and use thereof

A compound, morphinan technology, applied in the field of new analgesics, can solve the problems of low addiction and limited application, etc.

Inactive Publication Date: 2011-07-20
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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  • Heterocycle-fused morphinans compounds, preparation method and use thereof
  • Heterocycle-fused morphinans compounds, preparation method and use thereof
  • Heterocycle-fused morphinans compounds, preparation method and use thereof

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Experimental program
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Embodiment Construction

[0039] 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 reactions All 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; the silica gel used, including 200-300 mesh and GF254, were from Qingdao Products from Haiyang Chemical Factory or Yantai Yuanbo Silicone Co., Ltd.

[0040] 1. Preparation of Compound 2 (X=OMe, R=Me)

[0041] Method A: Preparation from compound 1 (X=OMe, R=Me):

[0042] Dissolve 1.1 g of the sulfate salt of compound 1 in 100 ml of H 2 O and 100ml of CH 2 Cl 2 In, use NH 3 .H 2 O adjusted the solution to basic (PH=10)....

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Abstract

The present invention discloses an aromatic or aliphatic heterocyclic condensed morphinan compound, a synthesis method thereof, and such applications thereof as opioid receptor agonist or anti-agonist in treating drug abuse and as novel painkiller. The general structural formula of the compound is shown in (I), wherein, R is H, straight chain or branch chain alkyl of C1 to C10, aromatic group or aliphatic heterocyclic or non-heterocyclic substituted alkyl; X is H, -OH, alkoxy, amido, substituted amido, carboxyl, ester group, aminoacyl; Y is H, -OH, alkoxyl, amido, substituted amido, etc., and Z is various substituted pentagon, hexagon or substituted pentagon, hexagon aromatic and aliphatic heterocycle.

Description

technical field [0001] The present invention relates to a class of aromatic or aliphatic heterocyclic condensed morphinan compounds, the synthesis method and its use as an opioid receptor agonist or antagonist for the treatment of drug abuse and brain dysfunction related to drug abuse, and as a novel Uses such as analgesics. 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, mol...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/18A61K31/485A61K51/04A61P25/04A61P25/36A61K101/02A61K101/00
Inventor 张翱
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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