State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, China.
Mar Drugs. 2021 Mar 31;19(4):198. doi: 10.3390/md19040198.
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.
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。
