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在相转移条件下,咔啉衍生物实施的环合反应,是对映纯吲哚喹嗪衍生物全合成中的重要进展之一;相同条件下,咔啉衍生物6S,R和6S,S环合,生成期待的吲哚喹嗪衍生物(7S,R,7S,S,8S,R,8S,S),表明这种类型的环合具有良好的适应性.在咔啉的3位引入羟甲基,不仅为吲哚喹嗪环提供了新功能基,还为进一步进行结构修饰奠定了基础;该功能基的引入使本文能成功地分离醛酮中间体9S,R和9S,S,为阐明上述环合反应机理提供了实验证据.
Under the condition of phase transfer, the cyclization reaction of carboline derivatives is one of the most important progresses in the total synthesis of enantiomer-pure indolquinolizines. Under the same conditions, carboline derivatives 6S, R and 6S, S To form the desired indolquinolizine derivatives (7S, R, 7S, S, 8S, R, 8S, S), indicating that this type of cyclization has good adaptability. Hydroxymethyl, not only provided a new functional group for indol-Quinolizine, but also laid the foundation for further structural modification. The introduction of this functional group led to the successful separation of aldehyde-ketone intermediates 9S, R and 9S, S, In order to elucidate the above mechanism of cyclization reaction provides experimental evidence.