Lactone compound of sweetsop connected through amido bond, synthetic method and application
A technology of annua lactone and a compound, which is applied in the field of synthesis of chiral annua lactone analogs, can solve the problems of poor water solubility, low synthesis efficiency, limited research progress of patent medicines and the like, and achieves a simple preparation method and high anti-cancer properties. active effect
Inactive Publication Date: 2010-12-22
SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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Problems solved by technology
In this series of compounds, the carbon skeleton of the molecule is constructed through the connection of ether bonds, which makes its synthesis efficiency not high; and the water solubility of this series of compounds is poor, which will limit the progress of its later drug research
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Abstract
This invention relates to an acetogenin compound linked by amide bonds, its synthesis method and its application. The acetogenin compound is an optically active or racemized compound, whose structural formula is shown in this invention, wherein, Y is C6-20 alkyl; n is 0-3; m is 7-19; R1, R2, R3 and R4 are the same or not, and are H or C1-10 alkyl; when n is 0-2, R3 and R4 are H, Cl, C1-10 alkyl or combined to form fiver-, six- or seven-membered ring shape; when n is 0, R1 and R2 are C1-10 alkyl or combined to form fiver-, six- or seven-membered ring shape. The acetogenin compound has high anticancer activity, and IC50 (mu.M) is lower than 0.04 to breast cancer (MDA-MB-435S). The can be manufactured into anticancer drugs. The synthesis method is simple, and suitable for industrial production.
Description
technical field The invention relates to a lactone compound, in particular to a synthesis method and application of a chiral anemone lactone analog connected by an amide bond. Background technique Currently, cancer has become the greatest threat to human health, and its incidence is increasing year by year. Cancer is responsible for more than 20% of all deaths each year, a figure that exceeds the combined number of deaths from AIDS, tuberculosis and malaria. Traditional cancer treatment methods, such as surgical resection, radiotherapy and chemotherapy, have certain defects, either incomplete treatment or severe side effects. With the development of modern organic separation identification and synthesis technology, many chemists are committed to the separation and identification of natural compounds with high anti-tumor activity and selectivity from natural products, and obtain this natural compound with relatively high content through organic synthesis. Low compounds, and...
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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/58A61K31/365A61K31/496A61P35/00
CPCY02P20/55
Inventor 姚祝军刘海侠张焕明
Owner SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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