Acta Chimica Sinica ›› 1999, Vol. 57 ›› Issue (3): 305-311. Previous Articles     Next Articles

Original Articles

8-葵炔基苯并内酰胺-V8的改良合成

马大为;王国强   

  1. 中国科学院上海有机化学研究所.上海(200032);中国科学院生命有机化学国家 重点实验室
  • 出版日期:1999-03-15 发布日期:1999-03-15

An improved synthesis of 8-decyl-benzolactam V8

Ma Dawei;Wang Guoqiang   

  1. Shanghai Inst Organ Chem., CAS.Shanghai(200032)
  • Online:1999-03-15 Published:1999-03-15

8-Decyl-benzolactam-V8 is a new protein kinase C (PKC) activator with some isoform-selectivity, and showes anti-cancer activity in vivo. This paper describes a new synthetic protocol for this compound. By using nitration product of L-phenylalanine derivative as starting material, we obtained the title compound in 22.4% overall yield. The key steps were iodination, DPPA-mediated cyclization and Pd/Cu- catalyzed coupling reaction of aryl iodide with 1-decyne.

Key words: LACTAM P, PALLADIUM, CUPRIC IODIDE, BENZENE P, IODIDE

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