examples of uses of 1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate_industrial additives

background and overview of examples of uses of 1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate

1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate is a fluorination reagent that can be used in electrophilic fluorination reactions. there are reports in the literature that it can be used to prepare favipiravir.

examples of uses and applications of 1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate

examples of uses and applications of 1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate 1.

cn202010583503.1 reported that 1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate can be useful for preparing favipiravir and its derivatives. specifically, compound a is used as the raw material, and a fluorine atom is selectively introduced at the 6-position through an electrophilic fluorination reaction to efficiently synthesize favipiravir or its derivatives, namely compound b, in one step. the general reaction formula is as follows:

where r1 is -conh2, -conh2, -conr3, -coor3, one of the cyano groups. benzylpyridine wherein r2 and r3 are h, c1-c6 alkyl, c1-c6 cycloalkyl, aryl-substituted alkyl. the above-mentioned one-step reaction refers to: placing compound a and fluorination reagent in a reaction solvent, and performing an electrophilic fluorination reaction at a certain temperature. the reaction temperature is 30-150°c, preferably 70-100°c. according to the above preparation method, the fluorinating reagent used in the electrophilic fluorination reaction includes but is not limited to n-f reagent. specifically, it includes: the fluorinating reagent used in the electrophilic fluorination reaction is selected from: n-fluorobenzene sulfonimide (nfsi), fluorobis(phenylsulfonyl)methane, n-fluoro-n-[4-(trifluoromethyl)phenyl]-(nfsa), 1-fluoro-4-hydroxy-1, 4-diazabicyclo[2.2.2]octane bistetrafluoroborate (accnfluor), 1-chloromethyl-4-fluoro-1,4-diazabicyclo[2.2.2]octane bis( tetrafluoroborate) salt (selectfluor), n-fluoropyridinium (tetrafluoroborate or triflate), 1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate, etc. .

examples of uses and applications of 1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate 2.

cn201610173119.8 reports an efficient synthesis method of 3-fluoro-fluorophenylboronic acid indole-2-carbonyl compound, including: in the presence of fluorinated reagents, solvents and additives, 3-hydrogen- indole-2-ol compounds undergo fluorooxidation reaction to obtain the corresponding 3-fluoro-indole-2-carbonyl compound. the fluorinated reagent is 1-chloromethyl-4-fluoro-1,4-diazabicyclo[2.2.2]octanebis(tetrafluoroborate) salt (fluorinated reagent), n-fluorobenzenesulfonate amide, 1-fluoro-2,4,6-trimethylpyridine trifluoromethanesulfonate, 1-fluoro-4-methyl-1,4-diazabicyclo[2.2.2]octane bis(tetrakis) fluoboric acid) salts of one or a mixture of several.

references

[1] [chinese invention] cn202010583503.1 preparation method of favipiravir and its derivatives

[2] [china invention, china invention authorization] cn201610173119.8 efficient preparation method of 3-fluoro-indole-2-carbonyl compound