Synthesis, physicochemical properties and biological studies of some substituted 2-alkoxy-4-methyl-morpholines

Article abstract of DOI:10.1016/0223-5234(89)90112-8

The title compounds have some structural characteristic of the piperidine-type analgesics and central sympathomimetics.The synthesis of some substituted 2-hydroxy- and 2-alkoxy-4-methyl-morpholines is presented and studied, in terms of electronic and steric effects.Their log P and pK_a values were determined and are explained in terms of structural, stereochemical and electronic effects.Acute toxicity and, for some selected cases, anti-nociceptive and central sympathomimetic activities have been evaluated in a preliminary (QSAR) study of biological properties of the synthesized compounds.