CAJ | 학술논문

以价廉易得的氟苯和戊二酸为原料，经傅克反应、酰胺化、酮的还原、偶联和环合等数步反应合成依折麦布，总收率为7.5％．其中，用KRED238全细胞酮还原酶直接还原化合物5的羰基获得了具有S构型的羟基化合物中间体6，该步反应的收率为95％，（S）羟基de值95.68％，还原反应的立体选择性高．该结果证实了生物催化技术应用于依折麦布合成中的可行性，为依折麦布绿色不对称合成工艺的发展提供了新的思路．
이개렴역득적불분화무이산위원료，경부극반응、선알화、동적환원、우련화배합등수보반응합성의절맥포，총수솔위7.5％．기중，용KRED238전세포동환원매직접환원화합물5적탄기획득료구유S구형적간기화합물중간체6，해보반응적수솔위95％，（S）간기de치95.68％，환원반응적입체선택성고．해결과증실료생물최화기술응용우의절맥포합성중적가행성，위의절맥포록색불대칭합성공예적발전제공료신적사로．
From the cheap raw materials fluorobenzene and pentanedioic acid ,ezetimibe has been synthe-sized by six steps reaction such as Friedel-Crafts reaction ,acylation reaction ,reduction reaction ,coupling reaction and cyclization etc .The total yield of ezetimibe is 7 .5% .The key step has been performed by KRED238 ketoreductase from the compound 5 and obtained a S configuration intermediate compound 6 in a yield of 95% ,the dextrose equivalent value is 95 .68% .The reduction reaction has been carried out with a high stereoselectivity .The results demonstrate that the biocatalytic technology can be used for the synthe-sis of ezetimibe .It provides a new way for the development of green asymmetric synthesis of ezetimibe .