期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 -, 期 -, 页码 -出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.2c00099
关键词
electrophilic reagents; fluorine; synthetic methods; difluoromethylation; library of S-([phenylsulfonyl]difluoromethyl)dibenzothiophenium salts
资金
- University of Rouen Normandy
- INSA Rouen Normandy
- Centre National de la Recherche Scientifique (CNRS)
- European Regional Development Fund (ERDF)
- Labex SynOrg [ANR-11-LABX-0029]
- Carnot Institute I2C
- graduate school for research XL-Chem [ANR-18-EURE-0020 XL CHEM]
- Region Normandie
- European Research Council (ERC) under the European Union's Horizon 2020 research and innovation program [758710]
- Region Normandy
An easy-to-handle protocol for synthesizing an efficient electrophilic (phenylsulfonyl)difluoromethylating reagent is described. The synthesized reagent is stable and safe for laboratory use, and a small library of electrophilic sources with varying counter anions is now available.
An easy-to-handle protocol for the synthesis of an efficient electrophilic (phenylsulfonyl)difluoromethylating reagent, namely, the S-([phenylsulfonyl]difluoromethyl)-dibenzothiophenium salt I, is depicted. The latter was synthesized on approximately 40 g scale in a three-step/one-purification sequence from commercially available or easy-to-synthesize starting materials with an estimated global prize of about 10.6 (sic)/g. The bench-stable reagent I was found to be air- and moisture-tolerant. By changing the counter anion, a small library of electrophilic sources (reagents I-III) is now available for the (phenylsulfonyl)difluoromethylation reaction. Differential scanning calorimetry (DSC) measurements have been also carried out on the different salts (I-III) along with a key intermediate to ensure a safe process.
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