Tyler, Jasper L. published the artcileStrain-Release Driven Spirocyclization of Azabicyclo[1.1.0]butyl Ketones, Quality Control of 5405-41-4, the main research area is azetidine spirocycle synthesis spirocyclization desilylation azabicyclobutane; strain release spirocyclization desilylation synthesis azetidine spirocycle; Azabicylo[1.1.0]butanes; Azetidines; Heterocycles; Spiro compounds; Strained molecules.
Due to their intrinsic rigidity, three-dimensionality and structural novelty, spirocyclic mols. have become increasingly sought-after moieties in drug discovery. Herein, we report a strain-release driven synthesis of azetidine-containing spirocycles by harnessing the inherent ring strain of the azabicyclo[1.1.0]butane (ABB) fragment. Novel ABB-ketone precursors bearing silyl-protected alcs. were synthesized in a single step and shown to engage in electrophile-induced spirocyclization-desilylation reactions. Primary, secondary and tertiary silyl ethers were effectively transformed into a library of new spiro-azetidines, with a range of substituents and ring sizes. In addition, the products are generated with synthetically useful ketone and protected-amine functional groups, which provides the potential for further elaboration and for this chem. to be utilized in the rapid assembly of medicinally relevant compounds
Angewandte Chemie, International Edition published new progress about Azabicyclic compounds Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (spirocycles). 5405-41-4 belongs to class esters-buliding-blocks, name is Ethyl 3-hydroxybutanoate, and the molecular formula is C6H12O3, Quality Control of 5405-41-4.
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