학술논문
Synthesis of 3,4-Fused Tricyclic Indoles through Cascade Carbopalladation and C–H Amination: Development and Total Synthesis of Rucaparib
Document Type
Article
Author
Source
Organic Letters; July 2020, Vol. 22 Issue: 13 p4985-4989, 5p
Subject
Language
ISSN
15237060; 15237052
Abstract
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.