Lipase-catalyzed resolution of 1-chloro-3-[(4-morpholin-4-yl-1,2,5-thiadiazole-3-yl)oxy]propan-2-ol: Synthesis of (R)- and (S)-timolol

Lipase-catalyzed resolution of 1-chloro-3-[(4-morpholin-4-yl-1,2,5-thiadiazole-3-yl)oxy]propan-2-ol (5) is described using vinyl acetate as acyl donor. The effect of different lipases from various sources in several solvents has been studied. This intermediate 5 is utilized in the preparation of enantiomerically enriched (R) and (S)-timolol.