Synthetic method for nicergoline

Abstract

The invention discloses a synthetic method for nicergoline. The synthetic method comprises the following steps: allowing lysergol and methanol to generate a methoxylation reaction, and carrying out purifying so as to obtain 10alpha-methoxyl-dihydrolysergol; allowing the 10alpha-methoxyl-dihydrolysergol and trimethylsulphoxonium iodide to generate a methylation reaction, and carrying out purifyingso as to obtain 1-methyl-10alpha-methoxyl-dihydrolysergol; and allowing the 1-methyl-10alpha-methoxyl-dihydrolysergol and 5-bromonicotinoyl chloride to generate an acylation reaction, and carrying outrefining so as to obtain the nicergoline. The synthetic method provided by the invention has the advantages of simple process, mild reaction conditions, easy operation, low toxicity of raw materials,high quality of a finished product, and facilitation of industrial popularization and application.

Description

technical field

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

[0002] Nicergoline, its chemical name is 10α-methoxy-1,6-dimethylergoline-8β-methanyl-5′-bromonicotinate, molecular formula C24H26BrN3O3, molecular weight 484.39, white to slightly yellow crystalline powder, Soluble in ethanol, hardly soluble in water, its structural formula is as structural formula 1:

[0003]

[0004] Nicergoline is mainly used clinically for the treatment of cognitive, emotional and behavioral disorders in the elderly, especially for vascular senile dementia. The pharmacological action of Nicergoline mainly acts on the α-receptor to cause vasodilation and is regarded as a vasoactive drug. In vitro studies, animal experiments and clinical trials in recent years have revealed its wide range of pharmacological effects and clinical application indications.

[0005] The technique of existing...

Images