1087-97-4Relevant articles and documents
Strategic Utilization of Multifunctional Carbene for Direct Synthesis of Carboxylic–Phosphinic Mixed Anhydride from CO2
Hoshimoto, Yoichi,Asada, Takahiro,Hazra, Sunit,Kinoshita, Takuya,Sombut, Panukorn,Kumar, Ravindra,Ohashi, Masato,Ogoshi, Sensuke
, p. 16075 - 16079 (2016)
Direct synthesis of carboxylic–phosphinic mixed anhydrides has been achieved by treating carbon dioxide with N-phosphine oxide-substituted imidazolylidenes (PoxIms) that contain both nucleophilic carbene and electrophilic phosphorus moieties. This novel mixed anhydride was efficiently derivatized into an ester, an amide, and an unsymmetrical ketone via transformation into its corresponding imidazolium salt followed by a dual substitution reaction. The presented work used well-designed multifunctional carbene reagents to establish a novel utility for carbon dioxide in organic synthesis.
Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis
Fu, Lei,Liu, Yuke,Lu, Yu,Sheng, Li,Wang, Bin,Zhang, Dongfeng,Zhao, Hongyi,Zhao, Wenting
, (2020/01/28)
A series of 4H-chromen-4-one derivatives obtained by scaffold morphing of the benzofuran compound, TAM16, were tested for antitubercular activity. Compound 8d was active against drug-sensitive and multidrug-resistant tuberculosis. A preliminary druggability evaluation showed that compound 8d displayed favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability. An in vivo study indicated that compound 8d exhibited modest efficacy in an acute mouse model of TB after 3 weeks of treatment. Thus, 8d is a promising antituberculosis lead compound.
Pd-catalyzed carbonylation for the construction of tertiary and quaternary carbon centers with sp3 carbon partners
Lu, Wei,Li, Yang,Wang, Chao,Xue, Dong,Chen, Jian-Gang,Xiao, Jianliang
supporting information, p. 5243 - 5249 (2014/07/08)
The first examples of a Pd-catalyzed carbonylation of aryl boronic acids with sp3 carbon partners are presented. Various boronic acids were shown to react with 1,3-diesters and 1,3-diketones to afford structurally unique carbonyl compounds. By