New composite method for triptolide

Abstract

The invention provides a new and effective method for asymmetrically compositing triptolide, belonging to the chemical composite field. The method takes 5-methoxyl-2-tetralone and 2-(2-iodine ethyl)-1, 4-butyrolactone as initial materials and composites the triptolide by chiral induction. The method is brief and convenient in operation and has high yield. As the reaction condition is mild, the composite method is easily industrialized and is further used for large-scale synthesis of target compounds.

Description

technical field [0001] The invention relates to a synthetic method of an organic compound, in particular to a synthetic method of triptolide. The structure of triptolide is shown in compound 1 in Formula 1. [0002] technical background [0003] Triptolide, also known as triptolide, is an active ingredient isolated from the traditional Chinese medicine Triptolide. Literature discloses that the compound has good antitumor activity, and the compound has also been found to have good activity in immunosuppression, male contraceptives, and the like. [0004] The synthesis of triptolide has been reported since 1977, and so far the following synthetic methods have been reported. [0005] Literature (G.A.Berchtold et al, J.Am.Chem.Soc., 1980,102,1200; J.Org.Chem., 1982,47,2364) discloses that 6-methoxy-1-tetralone is A method for synthesizing triptolide from starting materials (see formula 2). This method completes isopropylation through eight-step reaction, and obtains 6-iso...

AI Technical Summary

Problems solved by technology

Although this method provides the first asymmetric total synthesis of the target compound, the multi-step reaction yield is still very low, the operation is difficult, and the key asymmetric reaction selectivity of the method is not good.

In particular, the yield of this method is very low, so this reaction cannot be used to synthesize a large number of target compounds

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