embedded image which can be obtained by 1,4 addition of 2-oxoalkanoates or 2-oxocarboxylic acids onto the appropriate ketones. The present invention also relates to the use of the PigD protein for catalysis of 1,4 additions of 2-oxoalkanoates/-carboxylic acids, for example pyruvate/pyruvic acid or 2-oxobutyrate/2-oxobutyric acid, onto aliphatic, aromatic and heterocyclic α,β-unsaturated ketones. The 1,4 additions are effected here with CO2 elimination. The use of the PigD protein as a catalyst in the aforementioned 1,4 additions enables the synthesis of addition products with stereoactive centers these addition products being preparable with an enantiomeric excess of more than 80% ee. The aliphatic, aromatic and heterocyclic α,β-unsaturated ketones which are suitable for the process are represented by the general formula I:; embedded image "/> Use of the PigD protein for catalyzing 1,4-additions of 2-oxoalkanoates to α, β-unsaturated ketones
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Use of the PigD protein for catalyzing 1,4-additions of 2-oxoalkanoates to α, β-unsaturated ketones

机译:PigD蛋白在催化2-氧代链烷酸酯向α,β-不饱和酮的1,4-加成中的用途

摘要

The present invention relates to the preparation of compounds of the general formula II; embedded image which can be obtained by 1,4 addition of 2-oxoalkanoates or 2-oxocarboxylic acids onto the appropriate ketones. The present invention also relates to the use of the PigD protein for catalysis of 1,4 additions of 2-oxoalkanoates/-carboxylic acids, for example pyruvate/pyruvic acid or 2-oxobutyrate/2-oxobutyric acid, onto aliphatic, aromatic and heterocyclic α,β-unsaturated ketones. The 1,4 additions are effected here with CO2 elimination. The use of the PigD protein as a catalyst in the aforementioned 1,4 additions enables the synthesis of addition products with stereoactive centers these addition products being preparable with an enantiomeric excess of more than 80% ee. The aliphatic, aromatic and heterocyclic α,β-unsaturated ketones which are suitable for the process are represented by the general formula I:; embedded image
机译:本发明涉及通式Ⅱ化合物的制备。 “嵌入式图像” 可以通过在适当的酮上加成1,4的2-氧代链烷酸酯或2-氧代羧酸来获得。本发明还涉及PigD蛋白用于在脂肪族,芳族和杂环上催化1,4加成的2-氧代链烷酸酯/-羧酸,例如丙酮酸/丙酮酸或2-氧代丁酸酯/ 2-氧代丁酸的用途。 α,β-不饱和酮。 1,4加成在这里是通过CO 2 消除来实现的。在上述1,4加成中使用PigD蛋白作为催化剂能够合成具有立体活性中心的加成产物,这些加成产物可以以超过80%ee的对映体过量来制备。适用于该方法的脂族,芳族和杂环α,β-不饱和酮由通式I表示:; “嵌入式图像”

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