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Title
| - Combinatorial Liquid-Phase Synthesis of [1,4]Oxazepine-7-onesvia the Baylis−Hillman Reaction
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Abstract
| - A new method for the synthesis of [1,4]oxazepin-7-ones from readily available aldehydes and α-aminoalcohols was developed using the Baylis−Hillman reaction as the key step. To determine the scopeand limitations of the method, a mixture library was synthesized from six aldehydes and six α-aminoalcohols on the soluble polymer support poly(ethylene glycol) 5000 monomethyl ether (MeOPEG)via split synthesis and analyzed by GC−EIMS. Those oxazepines that were formed predominantlywere resynthesized in a parallel synthesis and fully characterized. Thus, we have shown that splitsynthesis on MeOPEG can be an efficient method to rapidly screen the substrate spectrum of anewly developed reaction sequence.
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