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.
Keywords: combinatorial chemistry, polymer bound reagents, polymer bound scavengers, heterocycles, library synthesis, polymer assisted solution phase synthesis, reductive amination, oxazepinones
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