Total Synthesis of Natural Products Possessing Multiple Bioactivities and Isolation of Their Activities

1. 已经完成了12种具有多种生物活性的天然产物的合成和开发，例如：(1)中枢神经作用和抗真菌产物ES242s；(2)抗真菌、降胆固醇和影响calbistrins的神经生长因子；(3)抗菌和抗肿瘤的幽门螺杆菌；(4)四大抗生素之一四环素；(5)抗肿瘤、抗菌喹诺乳素；(6)影响胰岛素受体、抗肿瘤、抗hiv的黄酮类药物。值得注意的是，利用^<15>N-NMR研究已经开发了一种新的方法来澄清结构-活性关系。结果，发现一些药用化合物比母体天然产物表现出更强的活性。新的合成方法已经开发出来。(1)钯催化剂催化三段式便捷法合成戊烯基苯酚；(2)由相应的羧酸直接制备醛类和酮类；(3)含四氢吡喃类、呋喃类天然产物及抗肿瘤抗生素、紫杉醇类、乌斯蒂霉素类的合成研究。

1. The total synthesis and developments of 12 kinds of natural products possessing multiple bioactivities have been accomplished : for examples : (1) central nervous affecting and antifungal products ES242s ; (2) antifungal, cholesterol lowering and nerve growth factor affecting calbistrins; (3) antibacterial and antitumor pyralomicins; (4) one of big four antibiotics, tetracycline ; (5) antitumor and antibacterial quinolactacins ; and (6) insulin receptor affecting, antitumor and anti-HIV, asterriquinones. Remarkably, a new methodology have been developed by using ^<15>N-NMR studies for clarification of the structure - activity relationship. As a result, several medicinally useful compounds were found to show stronger activities than the mother natural products.2. New sysnthetic methods have been delveloped. (1) synthesis of prenylphenols by convenient method combining three segments using palladium catalysts ; (2) direct preparation of aldehydes and ketones from the corresponding carboxylic acids ; (3) synthetic studies on natural products containing tetrahydro-pyrans and furans, and antitumor antibiotics, taxols and ustiloxins.