01359nas a2200169   4500008004100000022001400041245015800055210006900213260000800282300001200290490000700302520069000309100002300999700002001022700002401042856012301066       2024                        eng d  a1359-734500aFunctionalized quinolones and isoquinolones via 1,2-difunctionalization of arynes: synthesis of antagonist agent AS2717638 and floxacin key intermediates0 aFunctionalized quinolones and isoquinolones via 12difunctionaliz  cDEC  a133-1360 v613 a<p>
	Quinolones and isoquinolones are privileged scaffolds in synthetic/medicinal chemistry and drug discovery due to their unique chemical structures and intrinsic properties. Herein, we reveal a transition-metal-free approach for their synthesis from the reaction of dimethyl-2-((phenylamino)methylene)malonate with aryne precursors under mild conditions. The substrate scope is broad, accommodating a wide range of functional groups. The synthetic utility of the developed protocol has been demonstrated in the total synthesis of the potent antagonist agent AS2717638 and key intermediates of floxacin congeners. The gram-scale experiments illustrate its synthetic potential.</p>
1 aMahale, Sachin, D.1 aPrasad, Anamika1 aMhaske, Santosh, B.  uhttps://library.ncl.res.in/content/functionalized-quinolones-and-isoquinolones-12-difunctionalization-arynes-synthesis