Preparation method of vincamine

Abstract

The invention provides a green preparation method of vincamine, which comprises the following steps: (1) reduction: introducing a tabersonine methanol solution and hydrogen into a micro-channel reactor through a charging pump to react, and filtering, concentrating and extracting the reaction solution twice after the reaction is finished, thereby obtaining an extracting solution; (2) oxidation: catalyzing an organic phase in the extraction liquid in the step (1) by using peroxy acid to carry out oxidation reaction, neutralizing by using a sodium bicarbonate solution after the reaction is finished, extracting and concentrating; and (3) rearrangement: dissolving the concentrated solid obtained in the step (2) with ethanol, rearranging in the presence of a catalyst, adjusting the pH value after the reaction is completed, filtering, washing and crystallizing the filter cake, and separating out the solid, namely vincamine. The preparation method is safe, environmentally friendly and capable of achieving continuous production, the product purity is 99% or above, automatic equipment can be adopted for continuous production, and the industrial production efficiency is improved.

Description

technical field [0001] The invention belongs to the field of organic chemistry or medicinal chemistry, and relates to a preparation method of a compound, in particular to a green preparation method of vincamine. Background technique [0002] Vincamine (vincamine) is a main alkaloid in Vinca minor, and it is a quinine in the monoterpene indole alkaloids. Its chemical name is (3α, 14β, 16α)-14,15-di Hydrogen-14-hydroxyivorene-14-carboxylate methyl ester, white powder. In 1953, Schlittle and Furlenmeier isolated vincamine from V.minor. [0003] Vincamine is suitable for cerebrovascular sclerosis, brain insufficiency, and eye, ear, nose, and laryngeal vascular diseases. It is especially suitable for the early manifestations of progressive brain insufficiency, such as dizziness, headache, memory loss, fatigue, and inability to concentrate. In addition, it also has a certain effect on retinal vascular sclerosis and cochlear disorders caused by blood vessels such as dizziness an...

AI Technical Summary

Problems solved by technology

[0008] (1) When preparing vincamine, the reaction time is longer, the impurities are large, and the purity and yield of the product are not high enough;

[0009] (2) Batch-type production equipment is adopted, and there are many follow-up process steps, the degree of industrialization is low, and the production efficiency is low;

[0010] (3) There are too many safety hazards during the hydrogenation reaction, and the safe production cannot be guaranteed

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