Method for preparing triptolide

Abstract

The invention discloses a method for preparing triptolide. Triptonide, triptolide, tripdiolide and 2-epitripdiolide in common threewingnut roots are of very approximate structures, tripdiolide and 2-epitripdiolide are a pair of chiral isomers with large separation difficulties. In the prior art, the four compounds are separated all through repeated silica-gel column chromatography, however, repeated silica-gel column chromatography consumes a great amount of solvents and is poor in reproducibility, only applicable to slight separation in laboratories, and hard to popularize in industrial production. In conventional industrial production, only a macroporous resin is available as column chromatography in service. By adopting the method disclosed by the invention, triptonide, triptolide, tripdiolide and 2-epitripdiolide can be separated and prepared without repeated silica-gel column chromatography. On the basis of a common C18 chromatographic column, the HPLC (High Performance Liquid Chromatography) method disclosed by the invention is capable of effectively separating chiral isomers, namely tripdiolide and 2-epitripdiolide, and is low in cost and good in repeatability.

Description

technical field [0001] The invention belongs to the field of chemistry, and relates to a preparation method and a separation and analysis method of known compounds, in particular to a method for preparing triptolide ketone, triptolide, triptolide and 2-epitriptolide and triptolide The HPLC separation and analysis method of B and 2-epitriptolide. Background technique [0002] Studies have found that four chemical components with very similar structures in Triptolide have excellent anti-tumor activity, namely: triptolide ketone, triptolide, triptolide and 2-epitriptolide. The structural formula is as follows: [0003] [0004] From the chemical structure, it can be found that the structures of these four compounds are very close, wherein triptolide and 2-epitriptolide are a pair of chiral isomers. This makes the separation of these four compounds very difficult. The prior art relies on repeated silica gel column chromatography when separating these four compounds. Howeve...

AI Technical Summary

Problems solved by technology

This makes the separation of these four compounds very difficult

The prior art relies on repeated silica gel column chromatography when separating these four compounds. However, repeated silica gel column chromatography consumes solvent and has poor reproducibility. It is only suitable for a small amount of separation in the laboratory and is difficult to promote in industrial production.

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