Title: Communication: Polymer-Assisted Solution-Phase Synthesis of 4,5-Dihydro- 1,4-Benzoxazepin-3(2H)-Ones
Volume: 8
Issue: 7
Author(s): Ignacio Carreras, Jurgen Scherkenbeck and Christian Paulitz
Affiliation:
Keywords:
combinatorial chemistry, polymer bound reagents, polymer bound scavengers, heterocycles, library synthesis, polymer assisted solution phase synthesis, reductive amination, oxazepinones
Abstract: The polymer assisted solution phase (PASP) synthesis of 4,5-dihydro-1,4-benzoxazepin-3(2H)-ones is described. Using salicylic aldehydes, α-bromo acetic acid esters, and primary amines as broadly variable building blocks, the target molecules were obtained in a straightforward manner. The use of polymer bound reagents and scavengers greatly simplified workup, and avoided the use of protecting groups. A small library was prepared, showing the feasibility of the synthetic concept for the generation of larger sets of screening compounds.
