| Summary: | 碩士 === 國立成功大學 === 化學系 === 88 === Currently, there are five types of antihypercholesterolemic agents used in clinic. Among them, hydroxy-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor is the most commonly used. Triol acid and its lactone form, diol lactone, are important intermediates for the preparation of an antihypercholesterolemic agent such as Simvastatin. The goal of this thesis is to synthesize the diol lactone from lovastatin by chemical and enzymatic methods.
In chemical method, we used lithium hydroxide as a base to hydrolyze Lovastatin. The yield of diol lactone as a white solid is 87%. In enzymatic method, we first seeked out the enzyme which could hydrolyze Lovastatin sodium salt, and then we found out the best condition for the reaction which is at 27~37℃, pH 9, with 15% MeOH, and with final yield of 85% of diol lactone.
Although the yield of the enzymatic method is slightly lower then the chemical method, its product is simple and easy to handle, and the enzyme can be used again. Therefore preparation of diol lactone with enzymatic method has more advantages than with chemical method.
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