Loading patent…
AssigneeKureha Kagaku Kogyo Kabushiki Kaisha
InventorsEisaku Takahashi, Takashi Kimura, Satoru Kumazawa
Estimating the term…
This invention provides a process for producing an optically active 1,2-diol derivative by optical resolution. The optically active 1,2-diol derivative of the formula (I) which is capable of utilizing as an intermediate of fungicidal optically-active azole derivatives can be produced by esterifying a 1,2-diol derivative of the formula (I) as a substrate with a carboxylic acid derivative of the formula (II) as a reagent in the presence of a lipase as a catalyst. ##STR1## wherein R.sup.1 is C1-C5 alkyl group, C3-C7 cycloalkyl group or C1-C5 haloalkyl group, R.sup.2 is C1-C3 alkyl group substituted by a phenyl group which may have one or two halogen atoms and/or C1-C4 alkyl groups, C2-C3 alkenyl group substituted by a phenyl group which may have one or two halogen atoms and/or C1-C4 alkyl groups, or C1-C3 alkyl group substituted by a phenoxy group which may have one or two halogen atoms and/or C1-C4 alkyl groups, R.sup.3 is C1-C10 alkyl group or aryl group, and R.sup.4 is hydrogen atom, C1-C5 alkyl group, C2-C4 alkenyl group or COR.sub.3.
A process for producing an optically active 1,2-diol derivative of the formula (I) by optical resolution which comprises esterifying a 1,2-diol derivative of the formula (I) as a substrate with a carboxylic acid derivative of the formula (II) as a reagent in the presence of a lipase as a catalyst, ##STR3## wherein R.sup.1 is C1-C5 alkyl group, C3-C7 cycloalkyl group or C1-C5 haloalkyl group, R.sup.2 is C1-C3 alkyl group substituted by a phenyl group which has one or two halogen atoms, one or two C1-C4 alkyl groups, or one halogen atom and one C1-C4 alkyl group, C2-C3 alkenyl group substituted by a phenyl group which has one or two halogen atoms, or one or two C-1-C4 alkyl groups, or one halogen atom and one C1-C4 alkyl groups, or C1-C3 alkyl group substituted by a phenoxy group which may have one or two halogen atoms, one or two C1-C4 alkyl groups, or one halogen atom and one C1-C4 alkyl group, R.sup.3 is C1-C10 alkyl group or aryl group, and R.sup.4 is hydrogen atom, C1-C5 alkyl group, C2-C4 alkenyl group or COR.sub.3, provided that said halogen does not include astitine.
Dependencies are inferred from the claim text.