Method for synthesizing naloxone or naltrexone

A synthesis method and technology of naltrexone, which is applied in the field of pharmaceutical chemistry, can solve the problems of low reaction yield, environmental pollution, and serious injury to synthesis workers, and achieve increased reaction speed, no side reactions, and increased yield Effect
CN101955484AInactive Publication Date: 2011-01-26甘肃普安制药股份有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
甘肃普安制药股份有限公司
Publication Date
2011-01-26
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a method for synthesizing naloxone or naltrexone, which comprises the following steps of: dissolving thebaine in formic acid, uniformly stirring, dripping an oxidant, keeping the temperature of between 20 and 40 DEG C for 3 to 7 hours, displacing gas in a reaction vessel by inert gas serving as protective gas for 3 to 5 times, adding a metallic framework catalyst, displacing the gas by hydrogen for 3 to 5 times, keeping the temperature of between 25 and 45 DEG C and stabilizing a system for 7 to 13 hours to obtain a compound 2; reacting the compound 2 with acetic anhydride at the temperature of between 60 and 100 DEG C for 1 to 2 hours to obtain a compound 3; taking the inert gas as the protective gas, adding toluene, chloroformic acid-1-chloroethyl ester and potassium bicarbonate into the compound 3, heating to the temperature of between 75 and 100 DEG C and reacting for 20 to 40 hours, concentrating under reduced pressure until the system is fully dry, adding 10 percent hydrochloric acid, and heating and refluxing for 2 to 6 hours to obtain a compound 4; dissolving the compound 4 and at least one alkylation reagent in an organic solvent 1 and reacting with alkali at the temperature of between 50 and 100 DEG C to obtain a compound 5; and reacting the compound 5 with boron tribromide in an organic solvent 2 at the temperature of between -10 and 40 DEG C for 2 to 4 hours to obtain a compound 6, namely the naloxone or naltrexone.
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Description

technical field

[0001] The invention relates to the technical field of medicinal chemistry, in particular to a new synthetic route of naloxone or naltrexone. Background technique

[0002] The main component of naloxone and its chemical name are: 17-allyl-4,5a-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride dihydrate

[0003] Molecular formula: C 19 h 21 NO 4

[0004] Molecular weight: 327.37

[0005] At present, the synthesis method from oxycodone to naloxone is reported in Beijing Academy of Military Medical Sciences. The synthesis method is as follows:

[0006]

[0007] The disadvantage of this process is that when the compound generates compound 1, the reaction conditions are not easy to control, side reactions are prone to occur, and the yield of the reaction is not high;

[0008] In the production process from oxycodone to naloxone, the total yield of this process is about 40%, and a large amount of toxic solvents such as chloroform and dichloroethane were us...

Claims

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