Trost Barry M, Sharif Ehesan U, Cregg James J
Department of Chemistry , Stanford University , 333 Campus Dr. , Stanford , CA 94035 , USA . Email:
Chem Sci. 2017 Jan 1;8(1):770-774. doi: 10.1039/c6sc02849g. Epub 2016 Sep 12.
Efficient synthesis of versatile building blocks for enabling medicinal chemistry research has always challenged synthetic chemists to develop innovative methods. Of particular interest are the methods that are amenable to the synthesis of chemically distinct and diverse classes of pharmaceutically relevant motifs. Herein we report a general method for the one-pot synthesis of cyclic α-amido-ethers containing different amide functionalities including lactams, tetramic acids and amino acids. For the incorporation of the nucleotide bases, a chemo and regioselective palladium-catalyzed transformation has been developed, providing rapid access to nucleoside analogs.
高效合成用于支持药物化学研究的通用结构单元一直是合成化学家面临的挑战，促使他们开发创新方法。特别令人感兴趣的是那些适用于合成化学性质不同且多样的各类药学相关基序的方法。在此，我们报道了一种一锅法合成含有不同酰胺官能团（包括内酰胺、四元酸和氨基酸）的环状α-酰胺基醚的通用方法。为了引入核苷碱基，我们开发了一种化学和区域选择性钯催化转化方法，能够快速获得核苷类似物。
