New Spiro[cycloalkane-pyridazinone] Derivatives with Favorable Fsp³ Character

Abstract

The large originator pharmaceutical companies need more and more new compounds for their molecule banks, because high throughput screening (HTS) is still a widely used method to find new hits in the course of the lead discovery. In the design and synthesis of a new compound library, important points are in focus nowadays: Lipinski’s rule of five (RO5); the high Fsp3 character; the use of bioisosteric heterocycles instead of aromatic rings. With said aim in mind, we have synthesized a small compound library of new spiro[cycloalkane-pyridazinones] with 36 members. The compounds with this new scaffold may be useful in various drug discovery projects.

Keywords

• Friedel–Crafts reaction
• Grignard reaction
• Fsp³ character
• pyridazinones
• spiro[cycloalkane-pyridazinone]
• hydrazine