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Bicyclo[1.1.1]pentanes

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Items 1 to 15 of 159 total

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Bicyclo[1.1.1]pentanes are useful chemical tools for bioisosteric replacement of aromatic and lipophilic groups. Bicyclo[1.1.1]pentanes are rigid scaffolds with one or two exit vectors positioned in a linear manner, thereby mimicking the para substitution pattern on arenes or tert-butyl/lipophilic moieties.

Why Bicyclo[1.1.1]pentanes?

Bicyclo[1.1.1]pentanes have recently been highlighted in the scientific literature as useful chemical tools for bioisosteric replacement of aromatic groups. Bicyclo[1.1.1]pentanes are rigid scaffolds with two exit vectors positioned in a linear manner, thereby mimicking the para substitution pattern on arenes.

Bicyclo[1.1.1]pentanes are three-dimensional fragments and were shown to display equivalent or improved physico-chemical and pharmaco-kinetic properties compared to the arene groups they are replacing (Figure 1).1 Therefore, when the arene group is serving as a spacer/scaffold and is not involved in Pi interactions with the biological target, switching to the corresponding bicyclo[1.1.1]pentane is strongly recommended.

It has also been shown that mono-substituted bicyclo[1.1.1]pentanes can also serve as lipophilic group replacement and can be considered as bioisosteres of tert-butyl groups.2 Bicyclo[1.1.1]pentanes are now standard components of our LipoSwitch kits and services.3

Bicyclo[1.1.1]pentanes are now routinely used in drug discovery programs and the demand for these building blocks is growing exponentially. The recent scientific articles are prompting medicinal chemists to use them more, not only for their improved properties, but also for the chemical diversity and novel IP space that they offer.

Why SpiroChem?

SpiroChem is the world leader in the design, synthesis and manufacturing of bicyclo[1.1.1]pentanes. SpiroChem has developed new proprietary chemical techniques and cost-efficient synthetic routes that allow for their diversification and production on large scale.4 Most of the bicyclo[1.1.1]pentanes can be offered on multi-gram scale and up to kilogram scale, in a short lead time and are affordable to support your drug discovery programs and beyond.

SpiroChem can provide these advanced building blocks containing bicyclo[1.1.1]pentanes from our comprehensive catalog, but also design synthetic routes to new series that are fit for your applications and that will facilitate their introduction in your molecules of interest, thereby reducing the amount of synthetic work that needs to be done and allowing you to focus on high-value-added transformations. So do not hesitate asking us for derivatives of our catalog products!

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