依折麦布的酶法合成
发布时间：2019-06-15 16:29
【摘要】：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.
[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.
【作者单位】： 重庆医科大学药学院药物化学教研室;重庆医科大学第一临床学院;尚科生物医药有限公司;
【分类号】：R914.5
，
本文编号：2500356
[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.
【作者单位】： 重庆医科大学药学院药物化学教研室;重庆医科大学第一临床学院;尚科生物医药有限公司;
【分类号】：R914.5
，
本文编号：2500356
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