Natural products and privileged structures

该项目的主要目标是合成基于 对映体纯净、立体化学定义明确、新颖、用途广泛和有趣的分子 源自自然产品和特权结构或受其启发的脚手架。该项目的具体目标是： 1.以八元内酯天然产物为基础制备示范库， 通过闭环歧化(RCM)化学合成高效抗肿瘤药物八角菌素A，并评估其对人类癌细胞株的细胞毒活性。 2.开发了一类用于组合化学的新型离子降冰片烯基连接剂。 3.采用固相技术和溶液相技术相结合的方法制备曲尼霉素A类似物。 4.聚合物负载的膦盐、烯烃交叉歧化、低聚手性的利用 大环核构建过程中的助剂和聚乙二醇二氧杂环己烷 三环菌素A 5.开发新的化学方法来制备独特的含氮支架。 6.开发固相不对称合成的新型无迹连接物方法。

The main objective of this project is the synthesis of compound libraries based on enantiomerically pure, stereochemically well-defined, novel, versatile, and interesting molecular scaffolds that are derived from or inspired by natural products and privileged structures. The specific aims of this project are: 1. Prepare a demonstration library based on the eight-membered lactone natural product and powerful antitumor agent octalactin A via ring-closing metathesis (RCM) chemistry and evaluate the analogues for cytotoxic activity against human cancer cell lines. 2. Develop a new class of ionic norbornenyl linkers for combinatorial chemistry. 3. Preparation of trienomycin A analogues by combinatorial methods using both solid- and solution-phase technologies. 4. Utilization of polymer-supported phosphonium salts, olefin cross-metathesis, oligomeric chiral auxiliaries and PEG-supported dioxolanes during the construction of the macrocyclic core of trienomycin A. 5. Development of novel chemistry to prepare unique nitrogen-containing scaffolds. 6. Development of novel traceless linker methodology for solid phase asymmetric synthesis.