Abstract:
Methods of preparing a fluorinated substrate by combining potassium fluoride, a quaternary ammonium salt, and a substrate substituted with at least one chloro, bromo, sulfonyl, or nitro group to thereby provide the fluorinated substrate are disclosed.
Abstract:
Disclosed are mild temperature (e.g., from 0 to 80° C.) SNAr fluorinations of a variety of halide and sulfonate substituted aryl and heteroaryl substrates using NMe4F.
Abstract:
4-Amino-5-fluoro-3-halo-6-(substituted)picolinates are conveniently prepared from 4,5,6-trichloropicolinonitrile by a series of steps involving fluorine exchange, amination, halogen exchange, halogenation, nitrile hydrolysis, esterification, and transition metal assisted coupling.
Abstract:
Provided herein are processes for the preparation of 4-amino-5-fluoro-3-halo-6-(substituted)picolinates comprising a step of converting chloropicolinoyl chlorides to fluoropicolinoyl fluorides.
Abstract:
Disclosed are mild temperature (e.g., from 0 to 80° C.) SNAr fluorinations of a variety of halide and sulfonate substituted aryl and heteroaryl substrates using NMe4F.
Abstract:
Provided herein are fluoropicolinoyl fluorides and processes for their preparation. In some embodiments, provided herein is a process for the preparation of 5-fluoro-6-aryl-picolinoyl fluorides from chloropicolinoyl chlorides.
Abstract:
Provided herein are processes for the preparation of 4-amino-5-fluoro-3-halo-6-(substituted)picolinates comprising a step of converting chloropicolinoyl chlorides to fluoropicolinoyl fluorides.
Abstract:
Provided herein are fluoropicolinoyl fluorides and processes for their preparation. In some embodiments, provided herein is a process for the preparation of 5-fluoro-6-aryl-picolinoyl fluorides from chloropicolinoyl chlorides.
Abstract:
Methods of preparing a fluorinated substrate by combining potassium fluoride, a quaternary ammonium salt, and a substrate substituted with at least one chloro, bromo, sulfonyl, or nitro group to thereby provide the fluorinated substrate are disclosed.
Abstract:
A method for the preparation of anhydrous, alcohol-free tetramethylammonium fluoride is described. The method includes fluorination of tetramethylammonium chloride with potassium fluoride in an alcohol solvent, removal of insoluble potassium salts, and finally, removal of the alcohol solvent and replacement of it with an aprotic solvent.