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A kind of preparation method of icetexane type abietane diterpene

A technology of rosinane diterpene and diazomethane, which is applied in the field of pharmaceutical synthesis, can solve problems such as poor chemical selectivity, and achieves the effects of high selectivity, high yield, and wide popularization and application.

Active Publication Date: 2022-04-01
CENT SOUTH UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the above-mentioned method has poor chemoselectivity, and what is obtained is a mixture

Method used

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  • A kind of preparation method of icetexane type abietane diterpene
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  • A kind of preparation method of icetexane type abietane diterpene

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Embodiment Construction

[0046] The techniques, features and effects of the present invention will be described below in conjunction with examples. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all embodiments, based on the embodiments of the present invention, those skilled in the art without paying creative labor, all of which are obtained. The scope of the invention is protected.

[0047] The chemical reagents used in the following steps are all commercially available materials without further processing. Each step reaction yield is calculated as a column chromatography separation yield, and the steps are analyzed by the Qingdao silica gel, and the ethanol solution of sulfuric acid and phosphomolybolymolymented acid is heated after infiltration.

[0048] Nuclear magnetic spectrals were analyzed by Bruker Advance 500 (1H: 500MHz, 13C: 125MHz). The following abbreviations are used for splitting situations. S represents Singlet, D represents ...

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Abstract

The invention discloses a method for preparing an Icetexane-type abietane diterpene, which comprises the following steps: S1: adding carnosic acid to a methylation system, separating solid and liquid, and collecting the solid phase to obtain intermediate 2; S2: adding the obtained Add the intermediate 2 to the reduction system, separate the solid and liquid, collect the solid phase to prepare the intermediate 3; S3, add the intermediate 3 to the rearrangement system, separate the solid and liquid, collect the solid phase to prepare the Icetexane type abietane diterpene; the synthesis method of the present invention has the characteristics of short reaction time, high selectivity, high yield, large-scale preparation, and no need for protection in key steps, and can be widely popularized and applied.

Description

Technical field [0001] The present invention relates to the field of pharmaceutical synthesis, and more particularly to the preparation method of Icetexane rosinane diterpene. Background technique [0002] Icetexane rhenetteritone is a B-ring amplification rhenetterinary diiterpene ingredient, which has been reported that there is more than 70 species of natural products, distributed extensive distribution, and found in various sects. (-) - BARBATUSOL was selected from the Coleus Barbatus Bentham to give an Icetexane rosin alkane, animal experiments showed strong lower blood pressure. (-) - Barbatusol (CAS 88515-76-8) also exists in the Salvia przewalskii. [0003] (-) - Barbatusol is lower in the plant, mainly by synthetic methods. All Synthesis Based on Metal - mediated Raw Configuration Reaction Strategies. In the relevant technique, the Louis acid catalyzed molecular Four-Crafts cyclosis is synthesized by the Barbatusol embedded body; in addition, there is also a semi-allocat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C37/00C07C39/17C07C67/08C07C69/757
CPCC07C37/002C07C37/00C07C67/08C07C2603/26C07C2603/32C07C69/757C07C39/17
Inventor 邓旭周应军曹伟刘婷婷杨舒婷曾光尧
Owner CENT SOUTH UNIV
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