Decarboxylative trifluoromethylthiolation of lithium pyridylacetates was achieved using N-(trifluoromethylthio)benzenesulfonimide as the electrophilic trifluoromethylthiolation reagent. The reaction afforded the corresponding trifluoromethyl thioethers in good yield. Furthermore, the preparation of lithium pyridylacetates by saponification of the corresponding methyl esters and subsequent decarboxylative
Syntheses of substituted pyridines and fluorinated compounds, which are often pharmaceutical targets, are important objectives in organic chemistry. Herein, we found that decarboxylative fluorination of lithium 2‐pyridylacetates occur under catalyst‐free conditions. The phenomenon can be applied to one‐pot transformation of substitutedmethyl 2‐pyridylacetate to 2‐(fluoroalkyl)pyridine by decarboxylative
The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.
[EN] CERTAIN PLADIENOLIDE COMPOUNDS AND METHODS OF USE<br/>[FR] CERTAINS COMPOSÉS DE PLADIÉNOLIDE ET PROCÉDÉS D'UTILISATION
申请人:KEANEY GREGG F
公开号:WO2019199667A2
公开(公告)日:2019-10-17
The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.