Novel preparation method for nicergoline

Abstract

The invention discloses a novel synthesis method for the raw material medicine of nicergoline (shown in formula I). The novel synthesis method disclosed by the invention comprises the following steps of: reacting ergosterol with 5-bromonicotinate derivatives to generate carboxylic ester; then performing a photocatalytic reaction with methanol in an acidic condition; and then performing a methylation reaction with a methylation reagent to generate nicergoline. With the adoption of the novel synthesis method disclosed by the invention, the cumbersome operation of the methods disclosed by the existing patents is avoided, the used solvent is low in toxicity, and the yield is high. The novel synthesis method is beneficial to industrialized popularization and application.

Description

technical field

[0001] The invention relates to a new method for preparing nicergoline, which belongs to the technical field of chemical medicine synthesis. Background technique

[0002] Nicergoline has a good therapeutic effect on vascular dementia by expanding cerebral blood vessels and improving brain metabolism, especially for Alzheimer's disease (Alzheimer's disease, ie AD disease). With the intensification of urbanization and aging, the number of elderly people in China has exceeded 140 million, and the incidence of geriatric diseases is also increasing year by year. With the increase of residents' income, the requirements for the quality of life of the elderly have also increased. Under this trend, the demand for therapeutic drugs for mental diseases such as senile dementia has also increased significantly.

[0003] Nicergoline is a semi-synthetic ergot alkaloid derivative developed by Italy Aibao Pharmaceutical Factory. In its synthetic process patent declared in t...

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