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Method of preparing 14-hydroxy-7,8-dihydromorphone

A technology for dihydronormorphone and dihydronorcodeinone, which is applied in directions such as organic chemistry, can solve the problems of being unsuitable for large-scale production, high toxicity of boron tribromide, and high operating costs, and achieves low cost and simplification. Manipulation, effect of simplified reaction manipulation

Inactive Publication Date: 2007-09-12
FUDAN UNIV
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Problems solved by technology

[0005] In the prior art, the temperature of boron tribromide deoxymethylation reaction needs to be controlled below 10°C, and the atoms of compound I with multiple lone pairs of electrons are combined with one molecule of boron tribromide respectively, so boron tribromide The molar ratio of the dosage is as high as 7 times, the boron tribromide reagent itself is expensive, and the operation cost is high; in addition, boron tribromide is highly toxic and needs to be reacted in special equipment, which is not suitable for large-scale production

Method used

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  • Method of preparing 14-hydroxy-7,8-dihydromorphone
  • Method of preparing 14-hydroxy-7,8-dihydromorphone

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Embodiment 1

[0017] Compound I 10g (27.1mmol) was dissolved in 190ml of 20% hydrobromic acid, stirred at 118°C for 20h under nitrogen protection, cooled, and adjusted to alkaline with 25% ammonia water. Let stand, filter, wash with water, and dry to obtain 7.15g, yield 91%.

Embodiment 2

[0019] Compound I 10g (27.1mmol) was dissolved in 190ml of 25% hydrobromic acid, stirred at 118°C for 20h under nitrogen protection, cooled, and adjusted to alkaline with 25% ammonia water. Let stand, filter, wash with water, and dry to obtain 6.28g, yield 80%.

Embodiment 3

[0021] Compound I 10g (27.1mmol) was dissolved in 190ml of 30% hydrobromic acid, stirred at 118°C for 20h under nitrogen protection, cooled, and adjusted to alkaline with 25% ammonia water. Let stand, filter, wash with water, and dry to obtain 5.90 g, yield 75%.

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Abstract

This invention discloses a method for preparing 14-hydroxide-7, 8-One drop of morphine dihydro, which takes 14-acyloxy-17- Cyano-7, 8-dihydro - codeine drop one as the raw material, hydro-bromic acid as the deoxidation methyl and hydrolyzation reaction reagent to process14-acyloxy-7, 8-dihydro-morphia ketone.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a preparation method of 14-hydroxy-7,8-dihydronormorphone. Background technique [0002] Naloxone hydrochloride is a pure antagonist of opioid receptor μ subtype, which can completely block the combination of opioid narcotic analgesics and opioid receptors, and clinical small dose (0.4mg) intramuscular or intravenous injection can quickly reverse the morphine Analgesic and respiratory depressant effects of similar substances. Therefore, it is mainly used for acute poisoning and withdrawal treatment of morphine drugs (such as heroin, etc.), and is also a good tool drug for pharmacological research. In recent years, in clinical research, this product is also used in the treatment of schizophrenia, cerebral ischemic stroke, senile dementia, anti-shock, alcohol poisoning, obesity, congenital painlessness, infant asphyxia syndrome, habitual constipation and other diseases. treat. [0003] E...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D489/08
Inventor 仇缀百郑优丽卢美艳王星海
Owner FUDAN UNIV
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