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xiongwei3707

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Lignans in nature is the widespread presence of a class of natural products, which not only can be found in many plants, animals and even humans have found. Lignans many compounds have shown a strong biological activity, and often is some potential drugs. Therefore, the lignans work on various aspects of the wide concern. Aryl tetralin of lignans in podophyllotoxin has significant anti-tumor activity, which podophyllotoxin glucoside derivatives etoposide (VP-16) and teniposide (VM-26) is widely used in clinical. Therefore, the study podophyllotoxin intermediate synthesis method has an important academic value and application value.
Summary of main thesis is divided into two parts and experiment. In the first part of the system outlined in the following:
1) podophyllotoxin category bioactive substances Research. Podophyllotoxin exists primarily on the Berberidaceae perennial herb group podophyllotoxin Bajiaolian a subfamily, Sinopodophyllum emodi a mountain of leaves and grass is a foot of the plants. Podophyllotoxin and its derivatives are very good with significant biological activity, its clinical glucoside derivatives are widely used anticancer drug. As podophyllotoxin complex structures, and its long line of synthetic route widespread, low-yield shortcomings. Extracted from the plant was still is the primary means of podophyllotoxin. Therefore, the synthesis of podophyllotoxin has an important value.
2) podophyllotoxin strategy and the framework to build on the progress in recent years. Most rely mainly on the synthesis of several key ways to build podophyllotoxin C-18 frame. If Diels-Alder reaction, Tandem conjugate addition reaction. In recent years the study of podophyllotoxin mainly concentrated in the intermediate and Improved synthesis of new synthetic routes to explore two aspects.
Papers in the experimental part of our literature considered on the basis of the experimental exploration, and podophyllotoxin intermediates with the structural characteristics of a simple pepper aldehyde as the starting material, ¦Á, ¦Â-unsaturated carbonyl compounds are selective reduction lithium aluminum hydrogen reduction reaction as the key steps to have the Knoevenagel condensation, peracetic acid epoxy between chlorine and alkaline hydrogen peroxide epoxy, DCC condensation esterification reaction of the three podophyllotoxin intermediates. This intermediates can be more convenient synthesis of podophyllotoxin.
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