Methodology for the Synthesis of Nitrogen Heterocycles

描述（由申请人提供）：本研究计划的长期目标是开发海洋抗肿瘤生物碱Nakadomarin的合成策略。本论文还对海洋吲哚生物碱securine A/B、securamine A/B和chartelline A的合成进行了研究。最初的目标将缺乏苯环上的溴原子。将研究一系列具有被称为四氢喹啉的共同核心的抗肿瘤抗生素的合成，包括来莫霉素和沙夫霉素A。新的合成策略和方法将在这些调查的过程中进行研究，特别是通过叠氮化物捕获锍离子，水解后得到内酰胺。将筛选合成中间体，特别是与天然产物更相似的合成中间体，以评估生物活性。

DESCRIPTION (provided by applicant): The long term objectives of this research program are to develop a strategy for the synthesis of the marine antitumor alkaloid nakadomarin. Also it is intended to investigate the synthesis of the marine indole alkaloids, securine A/B, securamine A/B and chartelline A using a putative biomimetic strategy. The initial targets will lack the bromine atoms in the benzenoid ring. The synthesis of a range of antitumor antibiotics with the common core known as tetrahydroquinolines, including lemonomycin and saframycin A will be studied. New synthetic strategies and methodology will be studied in the course of these investigations, in particular the trapping of sulfonium ions by azide to give, after hydrolysis, lactams. The synthetic intermediates, particularly as they more closely resemble the natural products, will be screened to assess biological activity.