- An efficient construction of 4-OXO-4H-chromene-2-carboxylate derivatives via one-pot cascade reaction under solvent-free conditions
-
An efficient synthetic strategy to chromone derivatives from commercially available diethyl acetylenedicarboxylate and phenols via a one-pot cascade reaction has been developed. Performing the reaction using pyridine and polyphosphoric acid as the catalyst at room temperature and 90°C without any solvent gave the chromone derivatives in good to high yields at one time. A possible reaction pathway was also proposed and supported by the experiment. This protocol is environmentally friendly and metal-free, with advantages including short reaction times, convenient operation, and mild reaction conditions.
- Huang, Chao,Guo, Jia-Hui,Fu, Huang-Mei,Yuan, Ming-Long,Yang, Li-Juan
-
p. 1204 - 1211
(2015/07/15)
-
- NOVEL BIS-CHROMONE DERIVATIVES, METHODS FOR THEIR PREPARATION AND USES THEREOF
-
The invention relates to novel bis-chromone derivatives, methods for their preparation and their therapeutic application, especially in the treatment or prevention of disease involving mast cell activation, such as allergic disease. Provided is a compound according to the general Formula (I).
- -
-
Page/Page column 17
(2014/07/08)
-
- Design, synthesis, and inhibitory activity of potent, photoswitchable mast cell activation inhibitors
-
Allergic reactions affect millions of people worldwide. The need for new and effective antiallergic agents is evident, and insight into the underlying mechanisms that lead to allergic events is necessary. Herein, we report the design, synthesis, and activity of photoswitchable mast cell activation inhibitors. In mast cell degranulation assays, these inhibitors possess significantly greater potency than an original, chromone-based antiallergic agent. Furthermore, one of the photoswitchable inhibitors shows a significant difference in inhibitory activity between its two photoisomeric forms. Further optimization could ultimately lead to a photoswitchable compound suitable for studying mechanisms involved in allergic reactions in a novel manner, with activity addressable by light and with precise spatiotemporal control over events at the molecular level.
- Velema, Willem A.,Van Der Toorn, Marco,Szymanski, Wiktor,Feringa, Ben L.
-
supporting information
p. 4456 - 4464
(2013/07/19)
-
- Synthesis of 2-Acyl substituted chromanes and intermediates thereof
-
Novel processes for producing enantiomerically enriched and enantiomerically pure compositions of 2-acyl substituted chromane compounds, and 2-acylchromane compounds that are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors are disclosed. Further disclosed are processes for producing salts such as acid addition salts for such enantiomerically enriched compositions.
- -
-
-