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发展一种合成海洋抗肿瘤生物碱中腺素的策略。此外，还研究了采用仿生策略合成海洋吲哚类生物碱、安全A/B、安全胺A/B和查柳碱A的方法。最初的目标将缺乏苯环中的溴原子。将研究以四氢喹啉类药物为共同核心的一系列抗肿瘤抗生素的合成，包括柠檬霉素和萨弗霉素a。在这些研究过程中，将研究新的合成策略和方法，特别是叠氮化物对磺胺离子的捕获，使其在水解后得到内酰胺。合成中间体，特别是因为它们更接近天然产物，将被筛选以评估生物活性。

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.