• Synthesis of 2-Azabicyclo[n.2.0]alkane-Derived Building Blocks

    From left: Dr. O. O. Grygorenko, M. Kurkunov, Dr. A. V. Tymtsunik (Enamine Ltd., Taras Shevchenko National University of Kyiv, National Technical University of Ukraine, Ukraine)

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Synthesis of 2-Azabicyclo[n.2.0]alkane-Derived Building Blocks

Synthesis of 2-Azabicyclo[n.2.0]alkane-Derived Building Blocks: O. O. Grygorenko, M. Kurkunov, I. A. Levandovskiy, A. V. Tymtsunik
Synthesis 2018, DOI: 10.1055/s-0037-1609434


Conformationally restricted scaffolds are valuable structural units in drug design and discovery. One interesting option is represented by bicyclic cyclobutane-derived heteroaliphatic templates, which have recently attracted increasing interest in different therapeutic areas. Recently, a team of scientists from the Ukraine reported a practical approach to the title structural templates, which holds promise to enable a facilitated access to a range of bioactive drug candidates incorporating 2-azabicyclo[n.2.0]alkane units.

  • Synthese von 2-Azabicyclo[n.2.0]alkan-abgeleiteten Bausteinen

    Synthesis of 2-azabicyclo[n.2.0]alkane derivatives

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The authors said: “Our approach to 2-azabicyclo[n.2.0]alkanes is a remarkable demonstration of the powerful synthetic tool, namely, the Strecker reaction–intramolecular nucleophilic cyclization (STRINC) sequence, which is used for the preparation of bicyclic amino acids and diamine derivatives.”
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