Modular radical cross-coupling with sulfones enables access to sp 3 -rich (fluoro)alkylated scaffolds
Abstract
Fluorination is a burgeoning technique for fine-tuning the properties of pharmaceutical compounds. Unfortunately, the cross-coupling reactions widely used to make carbon-carbon bonds in drug research can be tripped up by fluorine substituents. Merchant et al. report a class of easily prepared, solid sulfone compounds that engage in nickel-catalyzed coupling of their fluoroalkyl groups with aryl zinc reagents. These sulfones considerably simplify the synthetic routes to fluorinated analogs that would previously have required multistep strategies focused strictly on the fluorination protocol.
Document Details
- Document Type
- Pub Defense Publication
- Publication Date
- Apr 06, 2018
- Source ID
- 10.1126/science.aar7335
Entities
People
- Cheng Bi
- Deng-hui Bao
- Gary M. Gallego
- Guanda Che
- Jacob T Edwards
- James J. Mousseau
- Lijie Sun
- Michael R. Collins
- Monika M. Kruszyk
- Olugbeminiyi O Fadeyi
- Phil Baran
- Philippe Nuhant
- Rohan R. Merchant
- Tian Qin
- Wenhua Qiao
Organizations
- Innovation Fund Denmark
- National Institutes of Health
- Pfizer
- Scripps Research
- United States Department of Defense