Natural Products Chemistry Division, North-East Institute of Science & Technology (CSIR), Jorhat 785 006, Assam, India.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):359-61. doi: 10.1016/j.bmcl.2009.10.097. Epub 2009 Oct 29.
Potent antimalarial compound artemisinin, 1 was bio-transformed to C-9 acetoxy artemisinin, 2 using soil microbe Penicillium simplissimum along with C-9 hydroxy derivative 3. The products were characterized using high field NMR and MS-MS data. The absolute stereochemistry of the newly generated chiral centers has been ascertained by COSY and 1D NOESY experiments. This is the first Letter of direct C-acetoxylation of artemisinin using microbial strains.
强效抗疟化合物青蒿素 1 经土壤微生物简单青霉转化为 C-9 乙酰氧基青蒿素 2 以及 C-9 羟基衍生物 3。利用高场 NMR 和 MS-MS 数据对产物进行了表征。通过 COSY 和 1D NOESY 实验确定了新生成的手性中心的绝对立体化学。这是首次使用微生物菌株直接对青蒿素进行 C-乙酰化。
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