【摘要】：以價廉易得的氟苯和戊二酸為原料,經傅-克反應、酰胺化、酮的還原、偶聯和環(huán)合等數步反應合成依折麥布,總收率為7.5%.其中,用KRED238全細胞酮還原酶直接還原化合物5的羰基獲得了具有S構型的羥基化合物中間體6,該步反應的收率為95%,(S)-羥基de值95.68%,還原反應的立體選擇性高.該結果證實了生物催化技術應用于依折麥布合成中的可行性,為依折麥布綠色不對稱合成工藝的發(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)科大學藥學院藥物化學教研室;重慶醫(yī)科大學第一臨床學院;尚科生物醫(yī)藥有限公司;
【分類號】：R914.5
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本文編號：2500356