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filingDate 2000-01-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2002-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2002534516-A
titleOfInvention Morpholine derivatives having blood lipid lowering activity and antioxidant activity
abstract (57) [Summary]nThe present invention relates to a compound of the formula I wherein R 1 = CH Two CH Three , R Two = CH Three , R Three , R Four = H, R Five = C 6 H Five (Compound 1) or R 1 = CH Two CH Two CH Two ONO Two , R Two = CH Three , R Three , R Four = H, R Five = C 6 H Five (Compound 2) or R 1 = H, R Two -R Three = (CH Two ) Four , R Four = H, R Five = C 6 H Five (Compound 3) or R 1 = CH Two CH Two CH Three , R Two -R Three  = (CH Two ) Four , R Four = H, R Five = C 6 H Five (Compound 4) or R 1 = CH Two CH Two CH Two ONO Two , R Two -R Three = (CH Two ) Four , R Four = H, R Five = C 6 H Five (Compound 5) or R 1 = H, R Two = CH Three , R Three -R Four = (CH Two ) Four , R Five = C 6 H Five (Compound 6) or R 1 = CH Two CH Two CH Three , R Two = CH Three , R Three -R Four = (CH Two ) Four , R Five = C 6 H Five (Compound 7) or R 1 = CH Two CH Two CH Two ONO Two , R Two = CH Three , R Three -R Four = (CH Two ) Four , R Five = C 6 H Five (Compound 8) or R 1 = CH Two CH Two CH Two ONO Two , R Two = CH Three , R Three , R Four = H, R Five = H (compound 9) or R 1 = H, R Two = p-NO Two -C 6 H Four -CH Two CH Two , R Three -R Four = H, R Five = C 6 H Five (Compound 10)] and their evaluation of antioxidant activity, blood cholesterol lowering activity and blood lipid lowering activity. The 2-hydroxymorpholine derivatives 3, 6 and 10 are synthesized by reacting the appropriate amino alcohol (22 mmol) and 2-bromo-4-phenylacetophenone or 2-bromoacetophenone (10 mmol) in ether and acetone for 15 hours at room temperature. You. The 2-alkoxy derivatives 1, 4 and 7 are synthesized by reacting the respective 2-hydroxy derivatives with an appropriate alcohol in acidic medium by refluxing. Compounds 2, 5, 8 and 9 react their respective 2-hydroxy derivatives with 3-bromopropanol in acidic medium by refluxing, and then react the 2- (3-bromopropoxy) derivative with silver nitrate in acetonitrile under reflux. And synthesized. The compounds of formula (I) significantly reduce plasma total cholesterol, triglyceride and LDL-cholesterol levels. Compounds of formula (I) have potent antioxidant activity. Compounds of formula (I) having the above effects are useful in the treatment of hypercholesterolemia, hyperlipidemia and atheroma.
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