A one-pot
strategy for α-keto amide bond formation have been
developed by using ynamides as coupling reagents under extremely mild
reaction conditions. Diversely structural α-ketoamides were
afforded in up to 98% yield for 36 examples. This reaction features
advantages such as practical coupling procedure, wide functional group
tolerance, and extremely mild conditions and has potential applications
in synthetic and medicinal chemistry.
An efficient base-promoted approach for the synthesis of pyrido[1,2-a]pyrimidinones from ynones and 2methylpyrimidin-4-ols have been developed via the CÀ N and CÀ C formation procedure. Diversely structural pyrido[1,2a]pyrimidinones were afforded in up to 95% yield for 29 examples. This reaction featured with advantages such as practical tandem procedure, wide functional group tolerance and metal-free conditions, which has potential application in synthetic and medicinal chemistry.
An efficient ring expansion strategy has been developed for the construction of cycloheptanones through C-C bond cleavage. The reactions take place with easily accessible starting materials, good functional group tolerance, and mild reaction conditions in the presence of Cs2CO3 without any metal or oxidant reagent. The transition-metal free insertions of alkynes into carbon-carbon σ-bonds of acenaphthenone initialized through intramolecular nucleophilic addition/ring-opening to furnish multifarious cycloheptanones, which has the potential to be widely utilized in organic synthetic chemistry.
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