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Multigram Synthesis of C4/C5 3,3-Difluorocyclobutyl-Substituted Building Blocks

Synthesis 2018, 50 (24), 4949-4957

DOI: 10.1055/s-0037-1610237

Ryabukhin S.; Melnykov K.; Granat D.; Volochnyuk D.; Grygorenko O.

An approach for the multigram synthesis of 3,3-difluorocyclobutyl-substituted building blocks (including carboxylic acid, amines, alcohols, azide, trifluoroborate ketone) is described. It is shown that, in most cases, ethyl 3,3-difluorocyclobutanecarboxylate is a convenient common synthetic intermediate to obtain the target derivatives. For preparation of 3,3-difluorocyclobutanol or -cyclobutanone, an alternative pathway via reaction of dichloroketene and tert-butyl or benzyl vinyl­ ether should be applied.

Multigram Synthesis of C4/C5 3,3-Difluorocyclobutyl-Substituted Building Blocks

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