3,5-difluoropyridine-2,6-diamine derivatives, methods of preparation and methods of preparing 3,5-difluoropyridine-2,6-diamine

By reacting compound 3 with a p-alkoxybenzyl-substituted 3,5-difluoropyridine-2,6-diamine derivative and removing the protecting group in the presence of acid, the shortcomings of high temperature and high pressure or palladium catalysts in the prior art are overcome, and the industrial production of 3,5-difluoropyridine-2,6-diamine with high yield and low cost is realized.

CN117185995BActive Publication Date: 2026-06-09SHANGHAI LINKCHEM TECHNOLOGY CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI LINKCHEM TECHNOLOGY CO LTD
Filing Date
2023-09-08
Publication Date
2026-06-09

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Abstract

This invention relates to the field of organic synthesis, specifically to 3,5-difluoropyridine-2,6-diamine derivatives, their preparation methods, and methods for preparing 3,5-difluoropyridine-2,6-diamine. The general formula for 3,5-difluoropyridine-2,6-diamine derivatives is: where R1 and R2 are independently selected from C1-C6 alkyl groups. The 3,5-difluoropyridine-2,6-diamine derivatives of this application, due to the selection of p-alkoxybenzyl substituents, particularly p-methoxybenzyl, on both amino groups, have unexpectedly shown significant production advantages compared to 3,5-difluoropyridine-2,6-diamine derivatives with benzyl substituents on the amino groups. Specifically, the p-methoxybenzyl-substituted 3,5-difluoropyridine-2,6-diamine exhibits extremely high selectivity in its production process, producing only a small amount (less than 7%) of monosubstituted compounds, or even none at all, during the reaction, thus allowing for very high yields.
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