Design and synthesis of highly efficient substrate compatible to chemo-enzymatic synthesis

在生物催化转化广泛应用的情况下，应着重阐述“底物分子技术”和“生物催化剂的探索”两条途径。 该方法的目的是找到最佳的底物结构和合成路线，这将是最大限度地有利于酶催化反应的选择性，和目标分子的总效率。 作为研究结果，实现了三个主题：1）探索立体选择性全细胞微生物高度和有效还原的α-卤代酮的结构; 2）开发糖恶唑啉和糖衍生物的结构，其提供区域和立体选择性转化如Ferrier反应所需的游离官能团。 在此基础上，开发了合成（R）-盐酸特布他林和稀有糖的新路线。

Under these circumstances that biocatalytic transformation is widely used, two approaches, the elaboration of "substrate molecular technology" and "quest of biocatalysts" should be emphasized. The aim of this approach is to find the optimized structure and synthetic routes of substrates, which would be maximally advantageous for both selectivity of enzyme-catalyzed reaction, and the total efficiency to target molecules. As the results through the research, three topics were achieved: 1) the exploration of the structure of alpha-haloketones which would be highly and efficiently reduced by stereoselective whole-cell microorganisms; 2) development of the structure of sugar oxazolines and glycal derivatives which serves free functional groups requisite for regio- and stereoselective transformation such as Ferrier reaction, were established. Based on them, new routes for (R)-terbutaline hydrochloride and rare sugars became available.