Method for artificially synthesizing galanthamine

A galantamine and chemical synthesis technology, which is applied in the direction of organic chemistry, can solve the problems of a large amount of lycoris and insufficient production of galantamine, etc., and achieve the effect of simple preparation method and small limitations

Inactive Publication Date: 2010-07-21
泰州市宝嵘新材料有限公司
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Problems solved by technology

However, at present, the extraction of galantamine is carried out by separating and extracting from domest

Method used

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Embodiment 1

[0007] In Example 1, the present invention adopts the following method: Step 1, Substitution reaction: Put 300ml of methanol solution and 50g (0.33mol) of isvanillin into the reactor, stir to dissolve at room temperature, and then add 52.8g (0.33 Mol), stirring at room temperature for 2 hours (tracking TLC: EtOAc / MSO=1: 2) for substitution reaction. After the reaction is complete, it is concentrated under reduced pressure to dryness, filtered and rinsed with water to obtain 76 g of wet 6-bromoisovanillin , Oven drying, get 68 grams of 6-bromoisovanillin; step two, ethylamination: put 300ml of ethanol and 50 grams (0.21 mol) of 6-bromoisovanillin into the reactor and stir to dissolve, add 34.5 dropwise at room temperature Gram tyramine ethanol solution (0.25 mole), stirred for 6-7 hours. Cool to -5°C, add 15.8 g (0.4 mol) of sodium borohydride, about 8 batches of sodium borohydride, this reaction is violent, there are a lot of bubbles, so it is not easy to add more sodium borohy...

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Abstract

The invention discloses a method for artificially synthesizing galanthamine, which uses isovanillin and bromine as the raw materials. After the raw materials are subjected to substitution reaction, the reaction and industrial chemicla tyramine are subjected to amination and formylation to obtain formamide, the formamide is subjected to reaction to obtain a derivative of racemic narwedine, the derivative of racemic narwedine is reduced into racemic narwedine, N-methylephedrine is used to reduce unsaturated ketone and tartaric acid is used to carry out resolution to obtain levogyrate galanthamine. The method not only can conveniently and rapidly prepare the galanthamine, but also adopts artificial preparation so as to have little limination in the preparation process.

Description

Technical field [0001] The invention relates to a method for artificially synthesizing galantamine. Background technique [0002] Galanthamine (galanthamine) is a highly selective cholinesterase inhibitor, easily tolerated, without hepatotoxicity. It was originally used clinically for the sequelae of polio and myasthenia gravis. Now it is used for the treatment of Alzheimer's disease. It also improves memory impairment caused by dementia patients and organic brain diseases. Studies have proved that the central nervous system is closely related to human learning and memory. The amount of acetylcholine in patients with senile dementia is reduced, and the decrease in cholinergic (AChE) is the main cause of senile dementia. Therefore, galantamine hydrobromide is an acetylcholinesterase inhibitor that increases the patient's choline level and is a treatment The first choice for the treatment of Alzheimer's disease. However, the current extraction of galantamine is separated from th...

Claims

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Application Information

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IPC IPC(8): C07D491/107
Inventor 高荣周彬
Owner 泰州市宝嵘新材料有限公司
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