Mono- and Difluoromethylation\nof 3(2<i>H</i>)‑Pyridazinones

A method for direct <i>N</i>-monofluoromethylation\nof\npyridazinones with <i>S</i>-monofluoromethyl-<i>S</i>-phenyl-2,3,4,5-tetramethylphenylsulfonium triflate is disclosed.\nA method for the <i>N</i>- and <i>O</i>-difluoromethylated\npyridazinones with TMSCF<sub>2</sub>Br as the only promising difluorocarbene\nprecursor is also reported. Substrates with various relevant functional\ngroups, including analogues of Lynparza, are tolerated under both\nmethods.

Publication Details

Journal
Figshare
Published
2024-09-12
DOI
https://doi.org/10.1021/acs.orglett.4c03002.s001
Primary Topic
Plant Pathogens and Resistance
Type
article
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Mono- and Difluoromethylation\nof 3(2H)‑Pyridazinones

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Plant Pathogens and Resistance
article

Mono- and Difluoromethylation\nof 3(2H)‑Pyridazinones

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Abstract

A method for direct <i>N</i>-monofluoromethylation\nof\npyridazinones with <i>S</i>-monofluoromethyl-<i>S</i>-phenyl-2,3,4,5-tetramethylphenylsulfonium triflate is disclosed.\nA method for the <i>N</i>- and <i>O</i>-difluoromethylated\npyridazinones with TMSCF<sub>2</sub>Br as the only promising difluorocarbene\nprecursor is also reported. Substrates with various relevant functional\ngroups, including analogues of Lynparza, are tolerated under both\nmethods.

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Plant Pathogens and Resistance
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Mono- and Difluoromethylation\nof 3(2<i>H</i>)‑Pyridazinones · Figshare (2024) | TGRS Research Map | TGRS