Morpholine derivs. prepn. - by reduction of corresponding halogen deriv. with metal hydride complexes

摘要

Morpholine derivs. (I; R' = H, lower alkyl, PhCH2) were prepd. by redn. of II (X = O, S) with metal hydride complexes. I were useful as consciousness hindrance-improving agents. In an example, 23 g 4-benzyl-2-(2-thenyl)phenoxymethyl)morpholin-5-one in C6H6 was added to 7 g LiAlH4 in Et2O with ice cooling and the mixt. refluxed 5 hr to give, after treatment with (CO2H)2, 23 g 4-benzyl-2-(2-(2-thenyl)-phenoxymethyl)morpholine (III) oxalate. Treatment of 3.8 g III with ClCO2Et and then with aq. Ba(OH)2 gave 1.6 g 2-(2-(2-thenyl)phenoxymethyl)morpholine.