Production of hair orchid

一种毛兰素、化合物的技术，应用在毛兰素的制备领域，能够解决技术要求高、不利大规模生产、原料石斛来源紧缺等问题

Inactive Publication Date: 2007-01-17
ZHEJIANG TIANHUANG MEDICINAL PLANT PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Because the above-mentioned extraction method has high technical requirements, and the source of its raw material Dendrobium is relatively scarce, it is not conducive to large-scale production.

Method used

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  • Production of hair orchid
  • Production of hair orchid
  • Production of hair orchid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] [embodiment 1] the chemical synthesis of Erianin

[0078] 1. Preparation of 3,4,5-trimethoxybenzyl alcohol

[0079] In a 250ml three-necked flask, add 15g (76.45mmol) of 3,4,5-trimethoxybenzaldehyde, 200ml of absolute ethanol, heat to 40°C to dissolve, then add 1.48g (38.23mmol) of sodium borohydride, and heat to reflux After 45min, TLC detection, after the reaction is complete, cool to room temperature, add 10ml (555.8mmol) of deionized water, after quenching, filter with suction, wash the filter residue with 20ml of absolute ethanol, after combining the filtrates, concentrate to dryness with a rotary evaporator , add 100ml of dichloromethane to dissolve, wash with 2N sodium hydroxide solution 50ml x 2, then wash with deionized water 50ml x 2, add appropriate amount of anhydrous magnesium sulfate to dry overnight. Filter, wash the filter residue with 20 ml of dichloromethane, combine the filtrates, and concentrate to dryness with a rotary evaporator to obtain 3,4,5-tr...

Embodiment 2

[0107] [embodiment 2] the chemical synthesis of Erianin

[0108] 1. Bromination of 3,4,5-trimethoxytoluene

[0109] Add 10mmol of 3,4,5-trimethoxytoluene into a 50ml three-necked flask, add 20ml of carbon tetrachloride, heat and stir to an oil bath of 82-84°C, reflux the reaction solution, and then add 10mmol of N-bromo A mixture of substituted succinimide (NBS) and 0.5 mmol benzoyl peroxide (BPO), the addition time is about 10 minutes, after the addition, continue to stir and react for 20 minutes, and then filter. The filtrate was washed with water and saturated sodium chloride solution, dried over anhydrous magnesium sulfate and filtered. The filtrate was evaporated to dryness and passed through a column to collect the most polar component to obtain the product 3,4,5-trimethoxybenzyl bromide.

[0110] 2. Reaction with triethyl phosphite

[0111] 10mmol of 3,4,5-trimethoxybenzyl bromide, 50mmol of triethyl phosphite, and 40ml of toluene were stirred and refluxed for 12hr. ...

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Abstract

Production of pilolanmide is carried out by taking 3,4,5-trimethoxy-benzene and isocoumarin as initial raw materials, bond reacting and hydrogenation reacting to obtain final product. It is cheap and convenient and can be used for industrial production.

Description

technical field [0001] The invention relates to a preparation method of erianin. Background technique [0002] Cancer has become the second killer of humans next to cardiovascular disease. Currently commonly used methods of anti-cancer chemotherapy and radiotherapy can cause serious adverse reactions to the human body. Experts at home and abroad have found that the traditional Chinese medicine Dendrobium has anti-tumor, anti-aging and blood vessel expansion effects, and its ethanol extract and its bibenzyl compounds have different degrees of anti-tumor activity in vivo. The active ingredients of Dendrobium have attracted attention at home and abroad. [0003] The research results of Wang Tianshan et al. (In vitro test of the growth inhibitory effect of chemical components in Dendrobium drumstick on K562 tumor cell line, Natural Product Research and Development, 1997, 9 (2), 1-3) showed that bibenzyl and phenanthrene compounds In vitro cultured mouse L 1210 Aggregation an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C43/253C07C41/26C07C49/255C07F9/28
CPCC07F9/4056C07F9/5442C07C41/30C07C41/26C07C41/20C07C45/64C07C41/22A61P35/00C07C43/23C07C43/225C07C43/215C07C47/575
Inventor 李亦平慈宏亮刘双喜
Owner ZHEJIANG TIANHUANG MEDICINAL PLANT PHARMA
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