Fluorinated cycloalkane building blocks are important structural motifs which become increasingly important in various areas, and most of all in drug discovery and agrochemistry. But, from the systematically enumerated functionalized gem-difluorocycloalkanes 1-11, only the synthesis of compounds type 6 (in a course of Maraviroc project) and partially compounds type 11 was industry developed. Also, the laboratory scale synthesis to type 9 compounds was elaborated. However the multigram production of these compounds remains questionable. Recently, we elaborated a promising for the further industrial scale up chemical routes to the compounds type 5, 6, 7, 8, 9 and 11. These investigations as well as pioneering lab-scale approaches to the C7 1-3 type compounds and type 10 building blocks will be discussed in the report.

Synthesis of medchem-relevant gem-difluorocycloalkane building blocks

2019 Spring National Meeting

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