Cryptochlorogenic acid preparation method

Abstract

The present invention discloses a cryptochlorogenic acid preparation method comprising the following steps: taking chlorogenic acid, dissolving the chlorogenic acid in methanol, then adding 1-2mol / L hydrochloric acid for the reaction while stirring for 6-8h, using a 1-2mol / L NaOH solution for adjusting pH to be neutral, concentrating, dissolved in methanol, filtering, concentrating under reduced pressure, adding water for dissolving, and filtering to obtain a filtrate; taking the filtrate for pretreatment by a reverse phase C18 column, washing with water, collecting a water washing solution, concentrating, centrifuging, filtering, and preparing cryptochlorogenic acid by reverse phase industrial preparative chromatography. According to the cryptochlorogenic acid preparation method, best acid conversion conditions and alkali neutralization reaction conditions can be obtained by screening by system experiments, the high purity cryptochlorogenic acid can be prepared by the reverse phase industrial preparative chromatography, and the method is high in yield and suitable for large-scale preparation, and achieves good technical results.

Description

technical field [0001] The invention relates to a preparation method of an organic acid, in particular to a preparation method of cryptochlorogenic acid. Background technique [0002] Cryptochlorogenic acid is 4-caffeoylquinic acid, which belongs to the monocaffeoylquinic acid compound and is an isomer of chlorogenic acid (3-caffeoylquinic acid). In recent years, scholars at home and abroad have conducted in-depth research on the pharmacological activities of caffeoylquinic acid compounds, and found that they have some important biological activities, such as antioxidant, anti-inflammatory, antibacterial, antiviral, inhibiting smooth muscle contraction, lowering blood lipids, etc. It has clinical application value and is expected to play an important role in the treatment of viral hepatitis and cervical cancer. However, at present, such compounds are only in the laboratory research stage, and there is no method and technology for large-scale preparation, which greatly limit...

AI Technical Summary

Problems solved by technology

However, there is a common problem in the above-mentioned studies. Cryptochlorogenic acid is discovered in the process of chemical composition research. These methods are not aimed at the isolation, purification and preparation of cryptochlorogenic acid. They are random, poor in reproducibility, and The separation and purification steps are cumbersome and not suitable for large-scale separation and preparation

In addition, due to the low content of cryptochlorogenic acid in plants, the amount isolated by phytochemical means is very small, which cannot meet the research and application of animal experiments.

At the same time, it is also reported that foreign scholars use chemical synthesis of cryptochlorogenic acid (Zhang Yamei. Synthesis of caffeoylquinic acid compounds[J]. Jiangxi Traditional Chinese Medicine, 2012,8(43):78.), but cryptochlorogenic acid The yield of selective esterification of quinic acid is very low, and the cost is high, the pollution is very large, and it has not entered large-scale production, and no one cares about it in China, all of which restrict its further development and application.

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