Synthesis, structure, and anticholinesterase activities of methylphosphonothionates of N-β-hydroxyethylmorpholine and N-β-hydroxypropylmorpholine
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The work was based on the interrelationship of the diastereomeric anisochromicity on the introduction of an asymmetric center outside the ring of the amino alcohol and the anticholinesterase activity of the compounds including a morpholine heterocycle. A method is described for obtaining the compounds presented. Physicochemical constants and a method of determining anticholinesterase activity are given. In the series of O-ethyl derivatives of these compounds significant activity with respect to acetylcholinesterase can be distinguished. The efficiency of the series tested is comparable with that of tetraalkylammonium salts. It has been shown that alkyl 1-methyl-2-morpholinoethyl methylphosphonothionates are present in solution in two optically isomeric forms in a ratio of 1:3.
KeywordsMorpholine Amino Alcohol Asymmetric Center Methylphosphonic Acid Anticholinesterase Activity
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