Cubane-containing building blocks
In 2016, chemists showed that replacing a benzene ring in the neurotropic compound Leteprinim with a skeleton of cubane beneficially affected activity and water solubility of the parent compound (Figure 1). Since then the cubane-containing building blocks are gaining high popularity in drug discovery projects, as mimics for the benzene ring (Figure 2).
Herein, we synthesized cubane-1,4-diester 1 in 100 g scale following the literature protocol, and used it for the synthesis of diverse cubane-containing building blocks (Schemes 1).
Currently, we have synthesized 6 cubane-containing building blocks, that are available in our EnamineStore on a gram scale
We also have designed a library of cubane-containing building blocks for drug discovery programs. These molecules can be synthesized upon request within 4-6 weeks.
- Piperazine Bioisosteres for Drug Design
- Sugar-like Building Blocks for Drug Design
- Cyclic Sulfonamides for Drug Design
- Morpholine Bioisosteres for Drug Design
- P(O)Me2-containing Building Blocks for Drug Design
- Saturated Bioisosteres of ortho-/meta-substituted Benzenes
- Saturated bioisosteres of para-substituted benzenes
- Sulfonyl fluorides (-SO2F)