6141-60-2Relevant articles and documents
Kondrat'eva et al.
, (1971)
Medvedskaya,L.B. et al.
, (1979)
Traceless solid-phase α-hydroxytropolone synthesis
D'Erasmo, Michael P.,Masaoka, Takashi,Wilson, Jennifer A.,Hunte, Errol M.,Beutler, John A.,Le Grice, Stuart F. J.,Murelli, Ryan P.
supporting information, p. 1789 - 1792 (2016/09/23)
α-Hydroxytropolones are established inhibitors of several therapeutically relevant binuclear metalloenzymes, and thus lead drug targets for various human diseases. We have leveraged a recently-disclosed three-component oxidopyrylium cycloaddition in the first solid-phase synthesis of α-hydroxytropolones. We also showed that, while minor impurities exist after cleavage and aqueous wash, the semi-crude products display activity in HIV RT-associated RNaseH enzymatic and cell-based assays consistent with pure molecules made in solution phase. These proof-of-principle studies demonstrate the feasibility of solid-phase α-hydroxytropolone synthesis and its potential to serve as a powerful platform for α-hydroxytropolone-based drug discovery and development.
A mild, convenient and efficient single-step method for the synthesis of polysubstituted furans via ammonium ylide routes
Fan, Mingjin,Guo, Lina,Liu, Xueyuan,Liu, Weimin,Liang, Yongmin
, p. 391 - 396 (2007/10/03)
A new and convenient cyclization method for the synthesis of polysubstituted furans in a single-step via ammonium ylide routes was reported. In this process, dimethyl acetylenedicarboxylate reacted with ammonium ylide to produce polysubstituted furan in the presence of anhydrous K2CO 3 at room temperature. It is very economical, environmentally friendly and very easy to carry out. Georg Thieme Verlag Stuttgart.
