PURPOSE: To obtain an optically active 1-aryl-1,3-propanediol useful as a raw material for producing an antidepressant, etc., by hydrolyzing a racemic 1- aryl-1,3-diacetoxypropane in the presence of lipase in water and isolating a dihydroxy derivative.
CONSTITUTION: A racemic 1-aryl-1,3-diacetoxypropane of formula I (X is F or H; Ac is acetyl)(e.g. 1-phenyl-1,3-diacetoxypropane) is hydrolyzed in the presence of lipase derived from a microorganism such as Pseudomonas fragi, Pseudomonas sp., Chromobacterium viscosum, Mucor pusillus, Aspergillus niger, etc., in water to give a mixture of compounds of formula II to formula IV, water is distilled away by vacuum distillation, the residual oil is subjected to liquid chromatography and the compound of formula IV is isolated to give an optically active 1-aryl-1,3-diacetoxypropanediol formula IV useful as a starting raw material for tomoxetine showing strong pharmaceutical activity as an antidepressant.
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YOSHIDA NAOYUKI
SUGIURA MITSUYO
KOIZUMI YASUYUKI
