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Method for the preparation of morphine compounds

The technology of a compound, morphine, is applied in the field of naloxone, which can solve the problems such as toxicity associated with thiols

Inactive Publication Date: 2010-10-20
SANOFI AVENTIS SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] The use of mercaptans is associated with a pronounced odor as with most mercaptans and with associated toxicity

Method used

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  • Method for the preparation of morphine compounds
  • Method for the preparation of morphine compounds
  • Method for the preparation of morphine compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0127] Example: Preparation of Naloxone Containing Low Content of α,β-Unsaturated Compounds

[0128] 15.08 g (0.046 mol) of crude naloxone base (obtained as follows: in NaHCO 3 In the presence of N-allylation of noroxymorphone hydrochloride with allyl bromide at 60 ° C, and then precipitated from water) into a 250 ml three-necked flask equipped with a thermometer and a magnetic bar, and then added 105ml of water and 9ml (0.06mol, 2eq) of concentrated sodium hydroxide solution (30%). The medium is stirred at ambient temperature until complete dissolution.

[0129] The medium was then added to a dropping funnel and then added dropwise to a three-necked flask containing 36 ml (0.27 mol, 8 equivalents) of concentrated sodium hydroxide solution (30%). The initial ambient temperature of the reaction medium, ie 21.6°C, reached 21.5°C at the end of the addition, and then the pH of the reaction medium was 14.4.

[0130] Stirring was continued for another 30 minutes at this tempera...

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Abstract

The present invention relates to a method for the preparation of morphine compounds comprising a low content of alpha,beta-unsaturated compounds, which comprises the steps of: (i) bringing the crude morphine compound into contact with a base, at a pH of greater than 13, under conditions which make possible the Michael addition reaction on the alpha,beta-unsaturated compound(s) present; (ii) separating the morphine compound from the reaction mixture; and (iii) if appropriate, separating the addition product formed, from the morphine compound. It also relates to a composition comprising at least 99% by dry weight of morphine compound, or of a pharmaceutically acceptable salt thereof, and an alpha,beta-unsaturated compound in a content of less than 100 ppm.

Description

technical field [0001] The present invention relates to a process for the preparation of morphine compounds, particularly naloxone, which contain low levels of α,β-unsaturated compounds. The invention also relates to the compositions thus obtained. Background technique [0002] Morphine and similar compounds such as codeine, hydrocodone, hydromorphone, naloxone, naltrexone, oxycodone and oxymorphone are used as active ingredients in analgesics. [0003] Naloxone base (CAS No. 465-65-5) is a derivative of morphine used as an active ingredient in a drug, especially for overdose therapy: Naloxone is administered to displace morphine from the receptors, thereby allowing The effects of morphine cease. [0004] Said compounds can be obtained by total synthesis, but in view of the molecular complexity, said synthesis usually starts from plant extracts, especially poppy extracts, from poppy pods or from poppy resin (opium). These extracts often contain structurally similar differ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D489/00C07D489/08A61K31/485C07B63/02A61P29/00
CPCC07B63/02C07D489/00C07D489/08A61P29/00
Inventor 阿兰·德卢巴拉
Owner SANOFI AVENTIS SA
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