State Key Laboratory of Applied Organic Chemistry , Lanzhou University , Lanzhou 730000 , China.
J Org Chem. 2018 Dec 7;83(23):14626-14636. doi: 10.1021/acs.joc.8b02440. Epub 2018 Nov 28.
Alkynes difunctionalization is a powerful strategy in organic synthesis that provides a convenient synthetic entry for internal alkenes. The main challenge in this field was considered to be the geometry control of the newly formed double bond (thermodynamically controlled or kinetically controlled). Herein, we report a novel procedure (through the cyclic compounds broken) to completely control the regioselectivity of olefins. The products, difluoroalkyl unsaturated β-amino acid derivatives, have potential applications in some important pharmaceuticals on account of the special nature of fluorine atoms.
炔烃双官能化是有机合成中的一种强有力的策略，为内部烯烃提供了一种方便的合成入口。该领域的主要挑战被认为是新形成的双键的几何控制（热力学控制或动力学控制）。在此，我们报告了一种新的方法（通过环状化合物的断裂）来完全控制烯烃的区域选择性。产物，二氟烷基不饱和β-氨基酸衍生物，由于氟原子的特殊性质，在一些重要药物中有潜在的应用。
