Studies On The Stucture, Synthesis And Bioactivity Of Derivatives Of Ent-kaurane Diterpene

In this thesis, the chemical constituents ofRubdosin rubescens (Ldbiatase) have been investigated and fifty-three derivatives of ent-kaurene diterpene, which have a-methylene cyclopentanone function in their molecule and show the antitumor activity, have been designed and prepared. Some derivatives were tested for antitumor activity and three compounds were found to have stronger activity than oridonin. The destination molecule OGP46 have been obtained. A mild and efficient neutral method for the cleavage of acetyl with dibutyltin oxide have been developed. This method is especially useful in the synthesis of glycosides containing base or acid seneitive multifunctional group.1. The chemical constituents of Rubdosia Rubescens have been investigated. Seven compounds have been isolated from the alcohol extract of the dry leaves. A new ent-kaurene-p-D-glucoside named enmenolide was isolated together with the known compounds oridonin, ponicidin, ursolic acid, 2a, 3p-dihydroxy-urs-12-ene-28-oic acid, lasiodonin and pedalitin. The structure of new compound was determined to be ent-7p, 20-expoxy -kaur-16-ene-lot, 6p, 7