A series of novel 2-amino-4H-pyran derivatives have been synthesized via a three-component reaction of α,β-unsaturated ketone derivatives, malononitrile, aldehydes in excellent yields, using DBU as a catalyst and et...A series of novel 2-amino-4H-pyran derivatives have been synthesized via a three-component reaction of α,β-unsaturated ketone derivatives, malononitrile, aldehydes in excellent yields, using DBU as a catalyst and ethanol as a cheap, safe, and environmentally benign solvent under mild conditions. Their antitumor activity was evaluated in three human tumor cell lines, including human colon cancer （HCT116）, human cervical cancer （Hela）. and non-small cell lung cancer （H1975）.展开更多
A simple and efficient cascade Michael/cyclization reaction of 3-aminoindolin-2-ones with enones/enals was identified for the synthesis of potentially biologically active 3＇,4＇-dihydrospiro[pyrrol-3,2＇-oxindoles], ...A simple and efficient cascade Michael/cyclization reaction of 3-aminoindolin-2-ones with enones/enals was identified for the synthesis of potentially biologically active 3＇,4＇-dihydrospiro[pyrrol-3,2＇-oxindoles], using DBU as an efficient catalyst and ethylene glycol as an environmentally benign solvent. More diverse 3＇,4＇-dihydrospiro[pyrrol-3,2＇-oxindoles] analog libraries were prepared in good yields（up to 97%）. The structure of 3＇,4＇-dihydrospiro[pyrrol-3,2＇-oxindoles] was confirmed by mass spectrometry analysis, NMR analysis and single crystal X-ray diffraction. The main advantages of this method include the availability of starting materials, simple experimental operation, short reaction time,as well as high yields observed.展开更多
文摘A series of novel 2-amino-4H-pyran derivatives have been synthesized via a three-component reaction of α,β-unsaturated ketone derivatives, malononitrile, aldehydes in excellent yields, using DBU as a catalyst and ethanol as a cheap, safe, and environmentally benign solvent under mild conditions. Their antitumor activity was evaluated in three human tumor cell lines, including human colon cancer （HCT116）, human cervical cancer （Hela）. and non-small cell lung cancer （H1975）.
基金Financial support for this work by the National Natural Science Foundation of China(No.81202403)West China HospitalChengdu Science and Technology Department Translational Medicine Innovation Foundation(No.ZH13039)
文摘A simple and efficient cascade Michael/cyclization reaction of 3-aminoindolin-2-ones with enones/enals was identified for the synthesis of potentially biologically active 3＇,4＇-dihydrospiro[pyrrol-3,2＇-oxindoles], using DBU as an efficient catalyst and ethylene glycol as an environmentally benign solvent. More diverse 3＇,4＇-dihydrospiro[pyrrol-3,2＇-oxindoles] analog libraries were prepared in good yields（up to 97%）. The structure of 3＇,4＇-dihydrospiro[pyrrol-3,2＇-oxindoles] was confirmed by mass spectrometry analysis, NMR analysis and single crystal X-ray diffraction. The main advantages of this method include the availability of starting materials, simple experimental operation, short reaction time,as well as high yields observed.
