phthalazine catalysts have been designed and synthesized for enantioselective halolactonization of prochiral dienoic acids. The scope of the reaction is evidenced by 17 examples of spiro α-exo-methylene-halolactones with up to 99.8% enantiomeric excess. The resulting enantio-enriched spiro halolactone products are found to exhibit potent antitumor effects. In addition, both antipodes of products with equally
已经设计并合成了
氨基酸衍生的
酞嗪催化剂,用于手性二烯酸的对映选择性卤代内酯化。反应范围由对映体过量高达99.8%的螺α-外-亚甲基-卤代内酯的17个实例证明。发现所得的对映体富集的螺卤代内酯产物表现出有效的抗肿瘤作用。另外,由于保证了一对对映异构体催化剂,因此可以得到具有同等优异的对映异构度的两种产品的对映体。