优化 Nannocystin A 规模化合成的两步反应。
Optimization of Two Steps in Scale-Up Synthesis of Nannocystin A.
机构信息
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, China.
出版信息
Mar Drugs. 2021 Mar 31;19(4):198. doi: 10.3390/md19040198.
Abstract
We have accomplished a 10-step (longest linear) total synthesis of nannocystin A on a four hundred milligram scale. The previously reported Kobayashi vinylogous Mukaiyama aldol reaction to connect C4 and C5 was unreproducible during the scaling up process. A more convenient and cost-efficient Keck asymmetric vinylogous aldol reaction was employed to improve this transformation.
摘要
我们已在四百毫克规模上完成了对纳诺菌素 A 的 10 步（最长线性）全合成。在放大过程中，先前报道的 Kobayashi 乙烯基 Mukaiyama 烯醇缩合反应在连接 C4 和 C5 时不可重现。我们采用了更方便、更经济的 Keck 不对称乙烯基烯醇缩合反应来改进这一转化。
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