SYNTHESIS OF AROMATIC ANTIBIOTICS AND ANTICANCER AGENTS

正丁醇、新霉素、6-脱氧-6-去甲基四环素的合成 类比和奥利文是这项提议的具体目标。诺加罗尔 和诺加拉霉素都是有效的抗癌药物。奥利文是 橄榄霉素，具有抗菌和抗癌活性。这个 四环素类似物应表现出更好的药代动力学特征 很多四环素。诺加罗和四环素的合成基础 是一个串联Claisen-Diels-Alder序列，它是在我们的 实验室。此外，一条非常直接的途径可以到达蒽环类药物 骨架进行了描述。它应该是建造许多 11-脱氧蒽环素类似物。

The synthesis of nogarols, nogalamycin, 6-deoxy-6-demethyl-tetracycline analogs and olivin are the specific aims of this proposal. The nogarols and nogalamycin are potent anticancer agents. Olivin is part of olivomycin, which exhibits antibiotic and anticancer activity. The tetracycline analogs should exhibit better pharmacokinetic character than many tetracyclines. The basis for the nogarol and tetracycline syntheses is a tandem Claisen-Diels-Alder sequence which was developed in our laboratory. Additionally, a very direct route to the anthracycline skeleton is described. It should be ideal for the construction of many 11-deoxyanthracycline analogs.