Synthesis method of Euphorbiaceae diterpene Peplanol A

Abstract

The invention discloses a synthesis method of Euphorbiaceae diterpene Peplanol A. The synthesis method belongs to the field of organic synthesis, and comprises the following steps: by taking a cycloheptenone derivative 2 as a reaction raw material, constructing a key tricyclic skeleton through key steps of Negishi coupling reaction, Diels-Alder reaction, series cyclization reaction catalyzed by titanium free radicals and the like; finally, the target product Euphorbiaceae diterpene Pepluanol A is obtained through later functional group conversion. The synthesis method disclosed by the invention is simple and convenient to operate, the product is synthesized by 17 steps, the condition is mild, and the total yield reaches 2.5% by controlling the reaction condition. The synthesis route is novel in design thought, the raw materials are cheap and easy to obtain, the compatibility of each important functional group is strong, a plurality of Euphorbiaceae diterpene structure derivatives containing the same 5/6/7 fused ring skeleton can be conveniently synthesized, and a foundation is laid for the structure-function relationship research of the compounds.

Description

A kind of synthetic method of Euphorbiaceae diterpene Pepluanol A technical field The invention belongs to the field of organic synthesis, be specifically related to a kind of synthetic method of Euphorbiaceae diterpene Pepluanol A. Background technique [0002] As the precious wealth of nature, natural products have played an important role in the development of human society. based on Drug development of natural products has always been a top priority in drug development. Statistics show that the clinical new drugs approved by the FDA over the years Of these, more than half are derived from natural products or their derivatives. my country has abundant natural product resources and a long history of traditional Chinese medicine. In theory, the combination of the two is of great significance for the development of new drugs with independent intellectual property rights. Medicinal plants from Euphorbiaceae are used to treat diseases such as asthma and psoriasis in t...

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Problems solved by technology

However, the amount of natural products obtained through isolation is usually very small and cannot be prepared in large quantities. Therefore, the total synthesis of natural products has become an important intermediate link between the discovery of active ingredients and the research of medicinal chemistry.

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