骨格多様性指向型合成戦略に基づくsp³原子含有ベンゾアザ/オキササイクルおよびペプチドミメティクスの効率的合成手法の開発

抄録

In recent years, the modality of pharmaceuticals has diversified but small molecule drugs are still important because they are easy to produce and can target intracellular molecules. Heterocycles have long been used as the main scaffold of drugs and often control the properties of the molecule such as three dimensionality, lipophilicity, metabolic stability, and toxicity. Transition metal-catalyzed cross-coupling reactions have enabled the introduction of various substituents on aromatic rings. On the other hand, establishment of efficient synthetic methods for the construction of various non-planar heterocycles remains an important pursuit. Herein, we report the development of efficient synthetic methods for sp³ atom-containing benzo-aza/oxacycles and peptide mimetics based on skeletal diversity-oriented synthesis.