74433-49-1Relevant academic research and scientific papers
Synthesis of 3,4-Fused Tricyclic Indoles through Cascade Carbopalladation and C-H Amination: Development and Total Synthesis of Rucaparib
Cheng, Cang,Zuo, Xiang,Tu, Dongdong,Wan, Bin,Zhang, Yanghui
supporting information, p. 4985 - 4989 (2020/07/04)
3,4-Fused tricyclic indole scaffolds are ubiquitous in bioactive natural products and pharmaceuticals. A new protocol for the synthesis of 3,4-fused tricyclic indoles has been developed through cascade carbopalladation and C-H amination with N,N-di-tert-butyldiaziridinone. The protocol allows access to a range of 3,4-fused tricyclic indoles, including those containing various linkers and fused with medium-sized rings. Rucaparib can be synthesized via this reaction, providing an advantageous synthetic method for the FDA-approved cancer medicine.
A mild inter- and intramolecular amination of aryl halides with a combination of CuI and CsOAc
Kubo, Tetsuji,Katoh, Chiharu,Yamada, Ken,Okano, Kentaro,Tokuyama, Hidetoshi,Fukuyama, Tohru
supporting information; experimental part, p. 11230 - 11236 (2009/04/11)
A unique combination of CuI and CsOAc was found to catalyze aryl amination under mild conditions. The reaction takes place at room temperature or at 90 °C with broad functional group compatibility. The intramolecular reaction was able to form five-, six-, and seven-membered rings with various protecting groups on the nitrogen atom. The scope of the intermolecular amination, as well as its applications to unsymmetrical N,N′-dialkylated phenylenediamines, was investigated.
A convenient synthesis of 1-benzyl-1,2,3,4-tetrahydroisoquinolines by combined Strecker/Bruylants reaction
Reimann, Eberhard,Ettmayr, Christian
, p. 1289 - 1295 (2007/10/03)
Strecker reaction of iodophenethylamines with phenylacetaldehydes afforded the corresponding α-aminonitriles, which on treatment with i-propyl magnesium chloride underwent a Bruylants reaction to give the title compounds. Their structures were deduced by NMR and by an independent preparation starting from papaverine. The educts were easily available by standard procedures. Springer-Verlag 2004.
