Preparation of new bicyclo[2.1.1]hexane compact modules: an opening towards to novel sp3-rich chemical space

07 September 2022, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

Among the valuable saturated bicyclic structures incorporated in newly developed bio-active compounds, bicyclo[2.1.1]hexanes are playing an increasingly important role, while being still underexplored from a synthetic accessibility point of view. Here, we disclose an efficient and modular approach toward new 1,2-disubstituted bicyclo[2.1.1]hexane modules. Our strategy is based on the use of photochemistry to access new building blocks via [2+2] cycloaddition. The system can readily be derivatized with numerous transformations, opening the gate to sp3-rich new chemical space.

Keywords

new chemical space
sp3-rich
bicyclo[2.1.1]hexanes

Supplementary materials

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Title
Preparation of new bicyclo[2.1.1]hexane compact modules: an opening towards to novel sp3-rich chemical space
Description
Among the valuable saturated bicyclic structures incorporated in newly developed bio-active compounds, bicyclo[2.1.1]hexanes are playing an increasingly important role, while being still underexplored from a synthetic accessibility point of view. Here, we disclose an efficient and modular approach toward new 1,2-disubstituted bicyclo[2.1.1]hexane modules. Our strategy is based on the use of photochemistry to access new building blocks via [2+2] cycloaddition. The system can readily be derivatized with numerous transformations, opening the gate to sp3-rich new chemical space.
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