SYNTHESIS AND ANTITUMOR ACTIVITY OF TERPENOIDS

拟议中的研究可分为三大类。它们是： (A)关于区域选择性、可逆性和机制的研究 手性亚苯基烯丙基阴离子与二元试剂的不对称加成反应 亲电体、烯酮和烯亚胺；(B)上述化合物的合成应用 由不对称全合成说明的反应 ()-戊烯、()-戊烯内酯、脱氧戊烯基葡糖醛和 杂环化合物和(C)紫杉素、紫杉碱和紫杉醇的全合成 紫杉醇通过新型的选择性硼辅助迁移反应 7-羟基-1-甲氧基双环[2.2.2]-2-辛烯。建议的合成如下 一般情况下，从而可以实现许多类比。每个模拟器都将是 使用体外组织培养系统测试抗肿瘤活性。一次 活性化合物被鉴定出来，它们将在活体动物身上进行测试 模特们。

The proposed research can be divided into three catagories. These are: (a) studies of the regioselectivity, reversibility and mechanism of the asymmetric addition reaction of chiral sulfinylallyl anions with ambident electrophiles, enones and enimines, (b) synthetic applications of the above reaction as illustrating by the asymmetric total syntheses of (+)-pentalenene, (+)-pentalenolactone, deoxypentalenylglucuron and heterocyclic compounds and (c) total syntheses of taxusin, taxinine and taxol via the novel selective boron-assisted migration reaction of 7-hydroxy-1-methoxybicyclo[2.2.2]-2-octenes. The proposed syntheses are general, thereby a number of analogs can be achieved. Each analog will be tested for antitumor activity using in vitro tissue culture systems. Once the active compounds are identified, they will be tested in vivo animal models.