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Multigram Synthesis of Advanced 6,6-Difluorospiro[3.3]heptane-derived Building Blocks

Eur. J. Org. Chem. 2020, in press

DOI: 10.1002/ejoc.202000432

Olifir O.; Chernykh A.; Dobrydnev A.; Grygorenko O.; Moroz Y.; Voitenko Z.; Radchenko D.

A convenient methodology for constructing 6,6‐difluorospiro[3.3]heptane scaffold – a conformationally restricted isostere of gem ‐difluorocycloalkanes – is developed. Alarge array of novel 2‐mono‐ and 2,2‐bifunctionalized difluorospiro[3.3]heptane building blocks was obtained through the convergent synthesis strategy using a common synthetic precursor – 1,1‐bis(bromomethyl)‐3,3‐difluorocyclobutane. The target compounds and intermediates were prepared by short reaction sequences (6–10 steps) on multigram scale (up to 0.47 kg).

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