抗肿瘤药物。274. 安痛定和隐石松类似物 E 环 SAR 研究的新合成策略。
Antitumor agents. 274. A new synthetic strategy for E-ring SAR study of antofine and cryptopleurine analogues.
机构信息
Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599-7568, USA.
出版信息
Org Lett. 2010 Apr 2;12(7):1416-9. doi: 10.1021/ol902819j.
Abstract
A new versatile synthetic methodology for the synthesis of enantiomerically pure natural phenanthroindolizidines and phenanthroquinolizidines has been established and described. Natural products R-antofine and R-cryptopleurine, as well as a novel E-ring expanded analogue 13c (E7), 12-oxo-S-antofine (17), and 12N-methyl-12-aza-S-antofine (18) were synthesized with the new method. This strategy will greatly facilitate future SAR studies on the natural alkaloids with E-ring variations.
摘要
建立并描述了一种新的通用合成方法，用于合成对映体纯的天然菲并吲哚里嗪和菲并喹啉里嗪。利用新方法合成了天然产物 R-阿替非宁和 R-隐石松宁，以及一个新型 E 环扩展类似物 13c（E7）、12-氧代-S-阿替非宁（17）和 12N-甲基-12-氮杂-S-阿替非宁（18）。该策略将极大地促进未来对具有 E 环变化的天然生物碱的 SAR 研究。
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