The ruthenium-catalyzed intermolecular cascade cyclization of aromatic acids with aromatic aldehydes, which involves the direct insertion of C–H bond into a polar C=O bond and the successive intramolecular nucleophil...The ruthenium-catalyzed intermolecular cascade cyclization of aromatic acids with aromatic aldehydes, which involves the direct insertion of C–H bond into a polar C=O bond and the successive intramolecular nucleophilic substitution, was developed for the synthesis of 3-substituted phthalides in good to excellent yields. This one-pot procedure characterizes in a short reaction time, the cheaper Ru(II) as a catalyst, readily available acids and aldehydes as starting materials, and water as the only theoretical by-product.These merits make the protocol an efficient and cost-effective route for the synthesis of 3-substituted phthalides.展开更多
NTrifluoromethyl and cyclopropyl substituted 2-isoxazolines were synthesized via a DBU-promoted domino reaction of β-trifluoromethyl-/β-cyclopropyl-substituted enones with hydroxylamine. The domino reaction consists...NTrifluoromethyl and cyclopropyl substituted 2-isoxazolines were synthesized via a DBU-promoted domino reaction of β-trifluoromethyl-/β-cyclopropyl-substituted enones with hydroxylamine. The domino reaction consists of a Michael addition and the followed cyclization. A wide range of 3-substituted 5-cyclopropyl-5-trifluoromethyl-2-isoxazolines were obtained in good to excellent yields under mild reaction conditions. The method could also apply to other trifluoromethyl-substituted enones.展开更多
An efficient strategy for the synthesis of a variety of 3-methyleneisoindolin-1-ones has been developed. The re- action proceeded from coupling of 2-iodobenzamides （or 2-bromobenzamides） and terminal alkynes via Cu...An efficient strategy for the synthesis of a variety of 3-methyleneisoindolin-1-ones has been developed. The re- action proceeded from coupling of 2-iodobenzamides （or 2-bromobenzamides） and terminal alkynes via Cu（OAc）2.H20/2,2＇-biimidazole catalyzed in DMF at 60 ~C and subsequent additive cyclization produced substi- tuted 3-methyleneisoindolin-1-ones in good to excellent yields.展开更多
基金supported by the National Science Foundation of China (21572122, 21376146)Shaanxi Innovative Team of Key Science and Technology (2013KCT-17)the Fundamental Research Funds for the Central Universities (GK201703019, GK 201601005)
文摘The ruthenium-catalyzed intermolecular cascade cyclization of aromatic acids with aromatic aldehydes, which involves the direct insertion of C–H bond into a polar C=O bond and the successive intramolecular nucleophilic substitution, was developed for the synthesis of 3-substituted phthalides in good to excellent yields. This one-pot procedure characterizes in a short reaction time, the cheaper Ru(II) as a catalyst, readily available acids and aldehydes as starting materials, and water as the only theoretical by-product.These merits make the protocol an efficient and cost-effective route for the synthesis of 3-substituted phthalides.
基金Supports from the National Natural Science Foundation of China (Nos. 21272257, 21274041 and 21474028)
文摘NTrifluoromethyl and cyclopropyl substituted 2-isoxazolines were synthesized via a DBU-promoted domino reaction of β-trifluoromethyl-/β-cyclopropyl-substituted enones with hydroxylamine. The domino reaction consists of a Michael addition and the followed cyclization. A wide range of 3-substituted 5-cyclopropyl-5-trifluoromethyl-2-isoxazolines were obtained in good to excellent yields under mild reaction conditions. The method could also apply to other trifluoromethyl-substituted enones.
文摘An efficient strategy for the synthesis of a variety of 3-methyleneisoindolin-1-ones has been developed. The re- action proceeded from coupling of 2-iodobenzamides （or 2-bromobenzamides） and terminal alkynes via Cu（OAc）2.H20/2,2＇-biimidazole catalyzed in DMF at 60 ~C and subsequent additive cyclization produced substi- tuted 3-methyleneisoindolin-1-ones in good to excellent yields.
