Optimization of Two Steps in Scale-Up Synthesis of Nannocystin A

Marine Drugs

Liang Wang¹  Yue Chen¹  Shaojie Miao¹  Wenjie Liu¹  Tingrong Zhang¹  Mingxiao Zhang¹ 

[1] State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, China;

关键词: total synthesis;    natural product;    nannocystin;    anti-cancer;    gram-scale;   

DOI  :  10.3390/md19040198

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown