Tetrahedron Letters p. 7101 - 7104 (1990)
Update date:2022-08-02
Topics:
Deeter, Jack
Frazier, Jeff
Staten, Gilbert
Staszak, Mike
Weigel, Leland
Reduction of 3-(dialkylamino)-1-aryl-1-propanones with a 2 : 1 complex of <(2R,3S-(+)-4-dimethylamino-1,2-diphenyl-3-methyl-2-butanol> (8) and lithium aluminum hydride (LAH) provided the corresponding 1,3-diaminoalcohols in high ee's (80-88percent).This process was developed and applied to the synthesis of LY248686 (1), a potent inhibitor of serotonin (5HT) and norepinephrine (NE) uptake.Absolute configurations have been established by single crystal x-ray analysis.
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