School of Pharmaceutical Sciences, University of Shizuoka , 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan, and Process Technology Research Laboratories, Pharmaceutical Technology Division, Daiichi Sankyo Co., Ltd. , 1-12-1 Shinomiya, Hiratsuka, Kanagawa 254-0014, Japan.
Org Lett. 2013 Oct 18;15(20):5370-3. doi: 10.1021/ol4026815. Epub 2013 Oct 2.
N-formylsaccharin, an easily accessible crystalline compound, has been employed as an efficient CO source in Pd-catalyzed fluorocarbonylation of aryl halides to afford the corresponding acyl fluorides in high yields. The reactions use a near-stoichiometric amount of the CO source (1.2 equiv) and tolerate diverse functional groups. The acyl fluorides obtained could be readily transformed into various carboxylic acid derivatives such as carboxylic acid, esters, thioesters, and amides in a one-pot procedure.
N-甲酰基糖精是一种易于获得的结晶化合物,已被用作 Pd 催化的芳基卤化物的氟羰基化反应中有效的 CO 源,以高产率得到相应的酰氟化物。该反应使用接近化学计量的 CO 源(1.2 当量),并能耐受多种官能团。所得到的酰氟化物可以在一锅法中很容易地转化为各种羧酸衍生物,如羧酸、酯、硫酯和酰胺。