Efficient Synthesis of New Chiral Synthons by Artificial Regulation of Biocatalysis and Development of Optically Active Drugs

1.光学活性化合物的合成我们设计并合成了一种使用的手性合成中间体，一种氮素骨架，一种五氟醚组，一种四苯ylporphyrin动力学，因此，这些分子的光学活性化合物是由脂质体和亚tilisin-catalyzed动力学解决方案准备的，或通过非对称还原使用含有高能量的碳基还原酶。我们发现，在核药理学添加剂中，通过协调和类固醇诱导剂可以控制地进行遗传学修饰。我们也合成了来自2-acyloxy-2-（五氟苯基）乙腈的新chiral 1，2-diol和1， 2氨基醇。Lipase-catalyzed reactions at非常低温度（）SY.++.（イエD1） and △△イD1（）SY.++。（エD1） values were calculated according to a theoretical equation. 3。使用面包师'年份和纯净的还原酶进行非对称还原，使用面包师'年份和碳基还原酶对各种有影响的光学活性酒精进行无害还原。在一般情况下，从面包师的年份中去除了比面包师的年份更高的效率更高的平衡率。

1. Synthesis of Optically Active CompoundsWe designed and synthesized useful chiral synthetic intermediates having an azirine skeleton, a pentafluorophenyl group, a tetraphenylporphyrin moiety and so on. Optically active compounds of these molecules were prepared by lipase- and subtilisin-catalyzed kinetic resolutions or by asymmetric reductions using carbonyl reductases with high enantioselectivities. We found that the diastereofacial selectivity in the nucleophilic addition to azirine derivatives can be controlled by coordination and steric hindrance. We also synthesized new chiral 1, 2-diol and 1, 2 amino alcohol from 2-acyloxy-2-(pentafluorophenyl)acetonitrile.2. Lipase-catalyzed reactions at very low temperature(]SY.++.〔ィエD1) and △△SィイD1(〕SY.++.〔ィエD1) values were calculated according to a theoretical equation.3. Enantioselective reduction using bakers' yeast and purified reductaseAsymmetric reductions using bakers' yeast and carbonyl reductases afforded various optically active alcohols. In general, the reductases purified from bakers' yeast showed higher enantioselectivity than the whole cell of bakers' yeast.