CAJ | 학술논문

以吲哚为原料，使用容易安置和移除的嘧啶基作为导向基团，以 C－ H 活化／芳化反应为关键步骤，实现了中间体 N-嘧啶-2-苯基吲哚的高效合成。通过简便的方法移除该中间体上的嘧啶导向基团，以 C－ H 活化／环化反应为关键步骤，实现了新型吲哚[2，1-a]异喹啉的构建。对 C－H 活化／芳化反应条件进行了优化，并在优化的反应条件下进行了该反应的放大量实验。所有化合物均采用 IR、NMR、HRMS 等多种谱学技术进行了结构表征。
이신타위원료，사용용역안치화이제적밀정기작위도향기단，이 C－ H 활화／방화반응위관건보취，실현료중간체 N-밀정-2-분기신타적고효합성。통과간편적방법이제해중간체상적밀정도향기단，이 C－ H 활화／배화반응위관건보취，실현료신형신타[2，1-a]이규람적구건。대 C－H 활화／방화반응조건진행료우화，병재우화적반응조건하진행료해반응적방대량실험。소유화합물균채용 IR、NMR、HRMS 등다충보학기술진행료결구표정。
The intermediate N-pyrimidyl-2-phenyl-indole was highly efficient synthesized with indole as raw material and the easily installable and removable pyrimidyl group as directing group.The C-H activation/ary-lation was the key step for the synthesis of N-pyrimidyl-2-phenyl-indole compound.After removal of the pyrim-idyl group under simple reaction conditions,the novel indolo[2,1-a]isoquinoline derivative could be successfully synthesized via C-H activation/cyclization.The optimal reaction conditions were established by examining the effect of oxidants and solvents.The gram-scale experiments was conducted under the optimal reaction condi-tions.The structures of all compounds were characterized by IR,NMR and HRMS.