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青蒿素的异戊烯二磷酸类似物的简明合成。

Concise synthesis of artemisinin from a farnesyl diphosphate analogue.

机构信息

School of Chemistry, Cardiff University, Park Place, Main Building, Cardiff CF10 3AT, UK.

School of Chemistry, Cardiff University, Park Place, Main Building, Cardiff CF10 3AT, UK.

出版信息

Bioorg Med Chem. 2018 Apr 1;26(7):1314-1319. doi: 10.1016/j.bmc.2017.03.068. Epub 2017 Apr 4.

Abstract

Artemisinin is one of the most potent anti-malaria drugs and many often-lengthy routes have been developed for its synthesis. Amorphadiene synthase, a key enzyme in the biosynthetic pathway of artemisinin, is able to convert an oxygenated farnesyl diphosphate analogue directly to dihydroartemisinic aldehyde, which can be converted to artemisinin in only four chemical steps, resulting in an efficient synthetic route to the anti-malaria drug.

摘要

青蒿素是一种最有效的抗疟疾药物,人们已经开发出许多合成它的长路线。青蒿素生物合成途径中的关键酶——阿莫地喹合酶,能够将含氧法呢基二磷酸类似物直接转化为二氢青蒿醛,后者只需经过四个化学步骤即可转化为青蒿素,从而形成了一条高效的抗疟药物合成路线。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9614/5930831/ed2c5447128f/fx1.jpg

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