Palladium-mediated synthesis of 1,1,2-triarylethanes. Application to the synthesis of CDP-840
作者:Yi-Shan Lin、Yi-Chun Kuo、Chun-Hsiung Kuei、Meng-Yang Chang
DOI:10.1016/j.tet.2017.01.030
日期:2017.3
β-hydroxy sulfones 3, and (3) palladium-catalyzed desulfonylative cross-coupling of the corresponding 5 with aryl iodides 4 in the presence of t-BuOK under warming DMF in acceptable yields. A facile synthesis of CDP-840 (1v) has been studied.
从β-酮砜2开始,开发了一种针对1,1,2-三芳基乙烷1的三步方案。进行以下过程的简便过程:(1)用NaBH 4还原2,(2)BF 3 ·OEt 2介导的β-羟基砜3的Friedel-Crafts反应,和(3)钯催化的脱磺酰基交联在t- BuOK存在下,在温和的DMF条件下,将相应的5与芳基碘化物4偶合,得到可接受的收率。已经研究了CDP-840(1v)的简便合成方法。