合成路线:The oxidation of khelline (I) with nitric acid gives khellinequinone (II),which is reduced with SO2 yielding khellinequinol (III).The condensation of (III) with epichlorohydrin (IV) affords the 2,3-epoxypropyl ether of khellinequinol (V) (1),which is condensed with benzylisopropylamine (VI) by heating at 110 C giving 3-benzylisopropylamino-2-hydroxypropyl ether of khellinequinol (VII).Finally this compound is debenzylated by reduction with H2 over Pd/C in methanol - acetic acid (1,2).Compound (V) can also be obtained by direct reaction of khellinequinol (III) with 3-(benzylisopropvlamino)-2-hydroxy-1-chloropropane (VIII) by means of NaH in refluxing ethanol (1,2).
参考文献标题:Synthesis and B-adrenolytic properties of some amino alcohol derivatives of furo [3,2-g]chromone
文献作者:Martin,M.; et al.
参考来源:Eur J Med Chem - Chim Ther 1974,9(5),563-570
合成路线:The oxidation of khelline (I) with nitric acid gives khellinequinone (II),which is reduced with SO2 yielding khellinequinol (III).The condensation of (III) with epichlorohydrin (IV) affords the 2,3-epoxypropyl ether of khellinequinol (V) (1),which is condensed with benzylisopropylamine (VI) by heating at 110 C giving 3-benzylisopropylamino-2-hydroxypropyl ether of khellinequinol (VII).Finally this compound is debenzylated by reduction with H2 over Pd/C in methanol - acetic acid (1,2).Compound (V) can also be obtained by direct reaction of khellinequinol (III) with 3-(benzylisopropvlamino)-2-hydroxy-1-chloropropane (VIII) by means of NaH in refluxing ethanol (1,2).
参考文献标题:Iprocrolol
文献作者:Castar,J.; Weetman,D.F.
参考来源:Drugs Fut 1978,3(11),816
产品链接: CAS No. 37855-80-4››