Methodology for the Synthesis of Nitrogen Heterocycles

描述(由申请人提供)：该研究计划的长期目标是开发一种合成海洋抗肿瘤生物碱Nakadomarin的策略。此外，我们还打算利用一种假想的仿生策略来研究海洋吲哚生物碱、安全卡宁A/B、安全卡那胺A/B和查特林A的合成。最初的目标将缺少苯环中的溴原子。将研究合成一系列以四氢喹啉为共同核心的抗肿瘤抗生素，包括来诺霉素和沙拉霉素A。在这些研究过程中，将研究新的合成策略和方法，特别是叠氮化物捕获硫离子，在水解后得到内酰胺。将对合成中间体进行筛选，以评估生物活性，特别是因为它们更接近于天然产品。

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.