Chemical Space Exploration of Oxetanes

Abstract

This paper focuses on new derivatives bearing an oxetane group to extend accessible chemical space for further identification of kinase inhibitors. The ability to modulate kinase activity represents an important therapeutic strategy for the treatment of human illnesses. Known as a nonclassical isoster of the carbonyl group, due to its high polarity and great ability to function as an acceptor of hydrogen bond, oxetane seems to be an attractive and underexplored structural motif in medicinal chemistry.

Kinetic Resolution of β-Alkyl Phenylethylamine Derivatives through Palladium-Catalyzed, Nosylamide-Directed C−H Olefination

“…Depiction of the synthesis of the compounds rac-1a and rac-1o-x . The compounds rac-1a or rac-1o-x were obtained from 1-indanone or 1-tetralone via the Witting reaction, borane reduction, azide reaction followed by the Staudinger reaction, and amino protection in 20–40% yields ( Scheme 5 and Scheme 6 ) [ 26 , 27 , 28 , 29 ].…”