期刊
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
卷 13, 期 -, 页码 1950-1956出版社
BEILSTEIN-INSTITUT
DOI: 10.3762/bjoc.13.189
关键词
fluorination; heterocycles; mechanochemistry; multistep; solid-state synthesis
资金
- Cambridge Reactor Design for a Ph. D. award
- Bolashak International Scholarship of the President of the Republic of Kazakhstan for a Scholarship award
- EPSRC First Grant Scheme [EP/P002951/1]
- chool of Chemistry at Cardiff University
- EPSRC [EP/P002951/1] Funding Source: UKRI
- Engineering and Physical Sciences Research Council [EP/P002951/1] Funding Source: researchfish
Solventless mechanochemical synthesis represents a technique with improved sustainability metrics compared to solvent-based processes. Herein, we describe a methodical process to run one solventless reaction directly into another through multistep mechanochemistry, effectively amplifying the solvent savings. The approach has to consider the solid form of the materials and compatibility of any auxiliary used. This has culminated in the development of a two-step, one-jar protocol for heterocycle formation and subsequent fluorination that has been successfully applied across a range of substrates, resulting in 12 difluorinated pyrazolones in moderate to excellent yields.
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