A series of 4-aryl-6-aryloxymethylmorpholin-3-one derivatives were synthesized very efficiently from readily available starting compounds in two steps. Ring opening reactions of epoxides with aniline compounds on alumina gave corresponding β-aminoalcohols (3). The resulting β-aminoalcohols were reacted with 2-chloroacetyl chloride to yield the desired 4-aryl-6-aryloxymethylmorpholin-3-one derivatives (5). All compounds 5 were assayed for inhibitory activity against A549 lung cancer cell growth, and the inhibitory effect of the novel morpholin-3-ones on cell viability was dose-dependent.

4-aryl-6-aryloxymethylmorpholin-3-one derivatives show dose-dependent inhibitory activity against A549 lung cancer cell growth, making them promising candidates for further research.

Paper

Facile Synthesis and Evaluation of Cell A549 Growth Inhibitory Activity of 4‐Aryl‐6‐aryloxymethylmorpholin‐3‐one Derivatives

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