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Synthetic method of nicergoline

A technology of nicergoline and a synthetic method, applied in directions such as organic chemistry, to achieve the effects of high yield, good quality, and simplified post-treatment process

Active Publication Date: 2020-05-08
JIANGSU HI STONE PHARMA
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0005] The technical problem that the present invention mainly solves is to provide a kind of synthetic method of nicergoline, can solve the above-mentioned problem that existing nicergoline exists when synthesizing

Method used

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  • Synthetic method of nicergoline

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Embodiment 1

[0027] (1) Photocatalytic addition reaction to form 10-methoxy-dihydroergot alcohol

[0028] Using ergot alcohol as the starting material, the addition of methanol and ethylenic bonds under strong acidic conditions is carried out by ultraviolet light catalysis, and the 9, 10 double bonds are added to form 10-methoxy-dihydroergo alcohol.

[0029] Specifically, according to the mass ratio of ergool:methanol:concentrated sulfuric acid of 1:4:1.8, 5kg of ergool was added to a 50-liter photocatalytic reaction kettle, and then 20kg of methanol was added, and the ergool was dissolved and clarified by stirring. Then dropwise add 9kg of concentrated sulfuric acid with a mass concentration of 98%, close the reaction kettle, turn on the ultraviolet lamp of 6kW power, keep the reaction temperature at 25~30°C, after reacting for 4 hours, take a sample, and detect the reaction through TLC, so that the raw material spot is less than The control spot with a concentration of 5% in the reaction...

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Abstract

The invention discloses a synthetic method of nicergoline. The synthetic method comprises the following steps: (1) photocatalytic addition reaction; (2) purification of 10-methoxy-dihydroergosterol; (3) methylation reaction; (4) purification of 10-methoxy-1, 6-dimethane-8-carbinol-ergoline; (5) esterification reaction; and (6) purifying of the nicergoline. According to the Synthetic method of thenicergoline, the mild photocatalytic addition, methylation and esterification reactions in the reaction process are adopted, and the raw materials and reagents with high safety are selected, so that the whole synthesis process is safe and controllable, the post-processing process is simplified, and the product obtained by the reaction is high in yield, high in purity, good in quality and suitablefor industrial production.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a method for synthesizing nicergoline. Background technique [0002] Nicergoline is a semi-synthetic ergot alkaloid derivative, which has α-receptor blocking effect and vasodilator effect, can strengthen the energy metabolism of brain cells, increase the utilization of oxygen and glucose, and promote the conversion of neurotransmitter dopamine to enhance Nerve conduction, strengthen brain protein biosynthesis, improve brain function. [0003] Nicergoline, whose chemical name is 10-methoxy-1,6-dimethylergoline-8-methanolyl-5-bromonicotinate, is a semi-synthetic ergot alkaloid derivative, the starting material is generally The routes of ergot alcohol and lysergic acid esters obtained from plant extracts or biological fermentation are very different due to the different selection of raw materials. [0004] At present, most of the routes of nicergoline are relatively complic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D457/02
CPCC07D457/02
Inventor 卫耿虎杨宇周振军史加桂王多平
Owner JIANGSU HI STONE PHARMA
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