105780-30-1Relevant articles and documents
Quinoxalin -2 (1H)-ketone compound and its preparation method and application
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, (2016/10/10)
The invention relates to a 1-substituted-6-methoxy-7-(3-morpholine propoxy) quinoxaline-2(1H)-ketone compound which is shown as the formula (I), preparation method and an application thereof. The benzodioxole is used as the raw material and subjected to nitration reaction for two times to produce the dinitration product: 5,6-dinitrobenzo[d][1,3] dioxacyclopentane, the 5,6-dinitrobenzo[d][1,3] dioxacyclopentane is subjected to ring opening under conditions of strong alkaline to obtain the ring opening product: 2-methoxy-4,5-dinitrophenol, the 2-methoxy-4,5-dinitrophenol and 4-(3-chloropropyl) morpholine are allowed to perform nucleophilic substitution, so as to obtain 4-(3-(2- methoxy-4,5-dinitrophenoxy) propyl) morpholine, the 4-(3-(2- methoxy-4,5-dinitrophenoxy) propyl) morpholine is reduced and allowed to perform ring closing reaction with ethyl glyoxalate to produce 6-methoxy-7-(3-morpholine propoxy) quinoxaline-2(1H)-ketone, and finally the 6-methoxy-7-(3-morpholine propoxy) quinoxaline-2(1H)-ketone is allowed to react with halogenated hydrocarbon containing substituents R under the alkaline condition, so as to produce the 1-substituted-6-methoxy-7-(3-morpholine propoxy) quinoxaline-2(1H)-ketone compound. The ketone compound has inhibition effect on EGFR kinase.(img file='DDA0000468270950000011.TIF' wi='928' he='416'/).
Nucleic acids internally-derivatized with a texaphyrin metal complex and uses thereof
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, (2008/06/13)
Texaphyrin metal complex-oligonucleotide and -oligonucleotide analog conjugates are provided where the texaphyrin is bound to an internal linkage of the oligonucleotide or oligonucleotide analog, the conjugates having catalytic activity for the hydrolysis of ribonucleic acid. Further, conjugates demonstrating catalytic turnover are described, the conjugates being especially effective under conditions where the concentration of RNA target exceeds that of available conjugate.
Phosphoramidite derivatives of macrocycles
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, (2008/06/13)
The invention is directed to phosphoramidite derivatives of macrocycles, such as porphyrins and expanded porphyrins, including sapphyrins and texaphyrins. The phosphoramidite derivatives are useful as intermediates in the preparation of macrocycle-oligonucleotide conjugates.
