• From left: Dr. Maciej Pudelko, Anna Jedrzejczak and Dr. Diego Carballa (Novartis Pharma AG, Switzerland)

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Novel Synthesis of Orthogonally Protected Diazaspiro[3.4]octane Analogues

Maciej Pudelko presents a novel synthesis of orthogonally protected diazaspiro[3.4]octane analogues.

Synthesis of Orthogonally Protected 2,6-Diazaspiro[3.5]nonane and 2,6-Diazaspiro[3.4]octane Analogues as Versatile Building Blocks in Medicinal Chemistry: M. Pudelko and co-workers Synlett 2015, 26, 1815–1818

Azaspiro compounds are attracting increasing interest in medicinal and biological chemistry, but their synthesis remains a challenging endeavor for chemists. Recently, Dr. Maciej Pudelko from the company Selvita S.A. (Cracow, Poland), in collaboration with researchers from Novartis Pharma AG (Basel, Switzerland), published a novel six-step synthetic approach to these interesting organic frameworks.

Dr. Pudelko said: “Central fragments that contain spirocyclic amines such as 2,6-diazaspiro[3.5]nonane and 2,6-diazaspiro[3.4]octane gain more and more attention in the medicinal chemistry community. For our purposes we were interested in developing a robust and cost-effective synthesis of multigram amounts of these two orthogonally protected building blocks.”

 

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