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US 5,334,534 AGranted
Enzymatic preparation of optically active propanolol and .beta.-adrenergic blockers using esterase
AssigneeThe Board of Governors for Higher Education, State of Rhode Island and Providence Plantations
InventorChing-Shih Chen
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Abstract
A computer modeling approach is taken to delineate the structural requirements of substrate molecules for biocatalytic turnover and enantioselective discrimination. This leads to an efficient enzymatic preparation of optically active propranolol. The acyl-sustituents on the alcohol and the secondary amine of propranolol play crucial roles in controlling the catalysis and enantiospecificity, respectively, of the enzymatic hydrolysis.
Claims2
A method for the synthesis of an enzymatic optically active propranolol which comprises:
- effecting an enzyme mediated enantioselective hydrolysis on a substrate of the formula:
- ##STR4## wherein the hydrolytic enzyme is cholesterol esterase, pig liver esterase or porcine pancrease esterase to form the corresponding (R) and (S) enantiomers;
- separating the diasteroisomers;
- and
- recovering the separated diasteroisomers.
2 more elements
Dependencies are inferred from the claim text.