Electrophilic ring fluorination of 3,5-disubstituted pyrazoles: application to the formal synthesis of a neprilysin inhibitor key intermediate
| Autor: | Phannarath Phansavath, Anne Westermeyer, Virginie Ratovelomanana-Vidal, Gérard Guillamot |
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| Rok vydání: | 2020 |
| Předmět: |
010405 organic chemistry
Chemistry Electrophilic fluorination Acetal General Chemistry 030204 cardiovascular system & hematology Ring (chemistry) 01 natural sciences Combinatorial chemistry Catalysis 0104 chemical sciences 03 medical and health sciences Formal synthesis chemistry.chemical_compound 0302 clinical medicine Yield (chemistry) Electrophile Materials Chemistry Neprilysin |
| Zdroj: | New Journal of Chemistry. 44:20535-20543 |
| ISSN: | 1369-9261 1144-0546 |
| Popis: | The access to a new family of unusual 4-fluorinated pyrazoles bearing acetal moities at the 3- or 5-position has been achieved by electrophilic fluorination using Selectfluor® with yields up to 67%. The unconverted starting material can be recovered and recycled. This reaction has been successfully applied to the formal synthesis of a key intermediate in the synthesis of neprilysin inhibitors with 42% overall yield (5 steps). |
| Databáze: | OpenAIRE |
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