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Ainsliatrimer B preparation method

A compound and reaction technology, which is applied in the field of preparation of ainsliatrimer B, can solve the problems of low yield, many steps in the synthesis method, and low yield, and achieve the effects of shortening the reaction steps, increasing the yield, and huge market value

Inactive Publication Date: 2015-01-28
CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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AI Technical Summary

Problems solved by technology

[0007] The above-mentioned extraction method has the disadvantages that the yield is low, the steps of the synthetic method are numerous, and the yield is low.

Method used

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preparation example Construction

[0036] A preparation method of ainsliatrimer B, comprising the steps of:

[0037] Step 1, using dehydrocressin as a starting material to prepare the compound of formula (I), which specifically includes the following steps:

[0038] a. The compound of formula (III) is oxidized at the allylic position under the action of an oxidizing agent to prepare the compound of formula (IV);

[0039] b, making the compound of formula (IV) undergo an oxidation reaction under the action of an oxidizing agent to prepare a compound of formula (V);

[0040] c, making the compound of formula (V) react with iodotrimethylsilane to prepare the compound of formula (VI);

[0041] d, reacting the compound of formula (VI) with the compound of formula (IV), through a series reaction, including Saegusa oxidation, intermolecular Diels-Alder cycloaddition and free radical-mediated allylic oxidation reaction, to prepare formula (I) compounds;

[0042] The synthetic route is:

[0043]

[0044] In step ...

Embodiment 1

[0056] [Example 1] The chemical synthesis of ainsliatrimer B

[0057] 1. Preparation of isozaluzanin C (IV)

[0058] In a 2L three-necked flask, add 2.5g (10.86mmol) of dehydrocresinolide, dissolve it in 360mL of chloroform, slowly add 9.4mL (63.73mmol) of 65% tert-butanol hydrogen peroxide solution dropwise under stirring, and then add Selenium dioxide 282mg (2.54mmol), after reacting at room temperature for 8h, the reaction solution was filtered with silica gel, the filter residue was washed with 100mL dichloromethane, concentrated to 100mL by rotary evaporator, washed with 50mL10% sodium hydroxide solution and 50mL×2 brine The concentrated solution was dried over anhydrous sodium sulfate, filtered, the filter residue was washed with 20 mL of dichloromethane, the filtrate was combined, concentrated to dryness, and column chromatography (petroleum ether: ethyl acetate = 8:1-2:1) was recovered to obtain the raw material. 1.0130 g of hydrocressin to obtain isozaluzanin C (IV),...

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Abstract

The invention discloses an ainsliatrimer B preparation method. In the preparation method, ainsliatrimer B is prepared from dehydrocostus lactone as a raw material mainly through oxidation reaction, Diels-alder reaction, and other steps, and the ainsliatrimer B is guaiacum lactone type sesquiterpenes lactone trimer, and can be extracted and separated from ainsliaea DC plant ainsliaea fulvioides. The study finds that the compound has certain inhibitory action on proliferation of human rectal cancer LOVO cells and human lung cancer A549 cells. The method is as follows: dehydrocostuslactone as a raw material, a compound (V) is obtained by 2 steps of reaction in the yield of 72.47%, then the ainsliatrimer B is prepared from the compound (V), the reaction process is greatly shortened, and the yield is raised.

Description

technical field [0001] The invention relates to a drug synthesis method, in particular to a preparation method of ainsliatrimer B. Background technique [0002] Tumor is one of the important causes of human death, and its prevention and treatment have become one of the top tasks in the study of major human diseases. Among them, drug therapy is one of the main treatment methods for tumors. When cancer patients receive radiotherapy and chemotherapy to kill tumor cells, most anti-tumor drugs also have considerable damage to the normal body due to the lack of selective effects. Inhibition of bone marrow hematopoietic function, gastrointestinal reactions, damage to liver and kidney tissues, low immune function, etc. Combining traditional Chinese medicine with radiotherapy and chemotherapy can not only reduce its side effects, but also significantly improve the curative effect on tumors. At present, some antineoplastic drugs are directly or indirectly derived from natural produ...

Claims

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Application Information

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IPC IPC(8): C07D493/20
CPCC07D493/20
Inventor 唐亚雄陈雨文
Owner CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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