發(fā)布時(shí)間：2019-06-15 16:29

【摘要】：以價(jià)廉易得的氟苯和戊二酸為原料,經(jīng)傅-克反應(yīng)、酰胺化、酮的還原、偶聯(lián)和環(huán)合等數(shù)步反應(yīng)合成依折麥布,總收率為7.5%.其中,用KRED238全細(xì)胞酮還原酶直接還原化合物5的羰基獲得了具有S構(gòu)型的羥基化合物中間體6,該步反應(yīng)的收率為95%,(S)-羥基de值95.68%,還原反應(yīng)的立體選擇性高.該結(jié)果證實(shí)了生物催化技術(shù)應(yīng)用于依折麥布合成中的可行性,為依折麥布綠色不對(duì)稱合成工藝的發(fā)展提供了新的思路.
[Abstract]:Efolib was synthesized from fluorobenzene and glutaric acid by Fourier-gram reaction, amidation, ketone reduction, coupling and cyclization. The overall yield was 7.5%. Among them, the carbonyl group of compound 5 was directly reduced by KRED238 whole cell ketone reductase to obtain hydroxyl compound intermediate 6 with S configuration. The yield of the reaction was 95%, the (S)-hydroxyl de value was 95.68%, and the stereoselectivity of the reduction reaction was high. The results confirmed the feasibility of biocatalytic technology in the synthesis of Yitumai cloth, and provided a new idea for the development of green asymmetric synthesis process of Yitumai cloth.
【作者單位】： 重慶醫(yī)科大學(xué)藥學(xué)院藥物化學(xué)教研室;重慶醫(yī)科大學(xué)第一臨床學(xué)院;尚科生物醫(yī)藥有限公司;
【分類號(hào)】：R914.5
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本文編號(hào)：2500356