“Conformational restriction” concept has already gained a considerable attention in medicinal chemistry. Scientists are looking more and more now on 3D-shaped saturated building blocks. In this context, intrinsically conformationally rigid bicyclic amines seem to be promising for drug discovery. For example, Belaperidone - a drug candidate of Abbott - bearing a residue of a bicyclic amine, reached phase II of clinical trials. In this work, we have rationally designed, synthesized and applied a library of novel/previously scarcely available diverse bicyclic amines in medicinal chemistry. The key synthesis step was photochemical [2+2]-cyclization. Details of the synthesis and application of the obtained compounds will be discussed.

[2+2]-photochemical synthesis and application of bicyclic amines: Advanced building blocks for medicinal chemistry

254th National Meeting (2017)

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