Year: 2026
Type: article
Abstract: Skeletal editing enables direct structural reorganization of molecular frameworks, providing a powerful strategy for rapid exploration of chemical space in lead optimization. Herein we report a mild, photoinduced skeletal editing strategy that converts furans into pharmacologically valuable pyridazines without external photocatalysts. Upon photoexcitation, the H-bonding electron donor–acceptor (EDA) complex formed between furan and hexafluoroisopropanol (HFIP) enables activation of molecular oxygen, generating reactive oxygen species that promote oxidative ring opening of furan to a 1,4-dicarbonyl intermediate, which subsequently condenses with hydrazine hydrate to afford pyridazines. The method displays broad substrate scope, tolerates complex and drug-derived motifs, and can be implemented to continuous-flow processing with enhanced efficiency and scalability. Skeletal editing enables direct structural reorganization of molecular frameworks, providing a powerful strategy for rapid exploration of chemical space in lead optimization. Herein the authors report a mild, photoinduced skeletal editing strategy that converts furans into pharmacologically valuable pyridazines without external photocatalysts.
Source: Nature Communications
Authors: Juan Tang, Pingyao Gan, Wenjing Li, Lin Peng, Guiyu Yang, Yuying He, Shikun Zhou, Ting Long, Chong Tian, Haiyan Fu, Shun Li
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $6,990
Funder: Sichuan University
OpenAlex ID: W7164137609