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A kind of damarene diol trimethanol compound, crystal form a and preparation method thereof

A technology of dammarene diol and alcoholate, which is applied in the direction of steroids, organic chemical methods, organic chemistry, etc., and can solve the problems that have not yet been searched for research reports on the crystal form of dammarene diol and its preparation method. Achieve the effect of good market prospect, good stability, and broaden clinical application

Active Publication Date: 2021-09-28
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Research reports on the crystal form of dammarenediol and its preparation method have not yet been retrieved

Method used

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  • A kind of damarene diol trimethanol compound, crystal form a and preparation method thereof
  • A kind of damarene diol trimethanol compound, crystal form a and preparation method thereof
  • A kind of damarene diol trimethanol compound, crystal form a and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 Preparation of dammarene diol trimethanolate crystal form A

[0042] Add 1 g of dammarene diol into 12 ml of methanol, ultrasonically dissolve it for 0.5 h, and filter it with suction. The sample liquid crystallizes naturally at room temperature for 36 h, filters, and vacuum-dries the filter cake to obtain the needle-shaped dammarene diol trimethanol crystal form. a.

Embodiment 2

[0043] Embodiment 2 Preparation of dammarene diol trimethanolate crystal form A

[0044] Add 1 g of dammarene diol into 5 ml of methanol, sonicate for 0.5 h, dissolve, and filter with suction. The sample liquid crystallizes naturally at room temperature for 12 h, filters, and vacuum-dries the filter cake to obtain the needle-shaped dammarene diol trimethanol crystal form. a.

Embodiment 3

[0045] The preparation of embodiment 3 dammarene diol trimethanol compound

[0046] Add 1 g of dammarene diol into 1 ml of methanol, sonicate for 0.5 h, dissolve, and filter with suction. The sample liquid crystallizes naturally at room temperature for 24 h, filters, and vacuum-dries the filter cake to obtain the needle-shaped dammarene diol trimethanol crystal form. a.

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Abstract

The invention discloses a dammarene diol trimethanol compound, crystal form A and a preparation method thereof. The present invention provides a crystal form A of dammarene diol trimethanol, and its X-ray powder diffraction pattern includes the following X-ray diffraction peaks shown at 2θ angles: 6.58°±0.2°, 13.35°±0.2° , 15.45°±0.2° and 20.18°±0.2°, 21.83°±0.2°. The preparation method of the invention is safe and convenient, and the prepared dammarene diol trimethanol or crystal form A has good dissolution, high bioavailability and good stability, is suitable for drug development, and has good market prospects.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, in particular relates to a dammarene diol trimethanol compound and its crystal form, and specifically discloses a preparation method thereof. Background technique [0002] Dammarenediol (Dammarenediol II) is a precursor for the synthesis of protopanaxadiol, which can be derived from protopanaxadiol. Cytochrome P450 participates in the hydroxylation of dammarenediol C12 to form protopanaxadiol, and the C6 site of protopanaxadiol is hydroxylated by cytochrome P450 to obtain protopanaxatriol. These two compounds are the main molecular framework of ginsenosides. [0003] [0004] Chinese patent CN201310129592.2 discloses a method for the biosynthesis of dammarene diol, in which a recombinant strain is constructed by means of genetic engineering to produce dammarene diol. [0005] Chinese patent CN201810781608.0 obtains the recombinant Saccharomyces cerevisiae which uses xylose to pro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00
CPCC07B2200/13C07J9/00
Inventor 梁红宝朱峰
Owner LUNAN PHARMA GROUP CORPORATION
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