Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114329
Abstract: The incorporation of the fluorine motif is a strategy widely applied in drug design for modulating the activity, physicochemical parameters, and metabolic stability of chemical compounds. In this study, we attempted to reduce the affinity… read more here.
Keywords: mao inhibitors; mao; fluorine atoms; affinity ... See more keywords
Rhodium(III)-Catalyzed Intramolecular Annulation and Aromatization for the Synthesis of Pyrrolo[1,2-a]quinolines.
Sign Up to like & getrecommendations! Published in 2023 at "Organic letters"
DOI: 10.1021/acs.orglett.3c00321
Abstract: A rhodium(III)-catalyzed protocol for the synthesis of pyrrolo[1,2-a]quinolines through intramolecular annulation of o-alkynyl amino aromatic ketones and subsequent aromatization is reported. This transformation builds the pyrrole and quinoline moieties of the pyrrolo[1,2-a]quinoline in one pot… read more here.
Keywords: intramolecular annulation; pyrrolo quinolines; rhodium iii; synthesis pyrrolo ... See more keywords
Regioselective ring expansion followed by H-shift of 3-ylidene oxindoles: a convenient synthesis of N-substituted/un-substituted pyrrolo[2,3-c] quinolines and marinoquinolines
Sign Up to like & getrecommendations! Published in 2019 at "RSC Advances"
DOI: 10.1039/c9ra07831b
Abstract: Herein, we report a simple and metal-free protocol for the synthesis of 4-oxo-4,5-dihydro-3H-pyrrolo[2,3-c]quinolines. read more here.
Keywords: regioselective ring; ring expansion; expansion followed; pyrrolo quinolines ... See more keywords
Catalyst-Free Synthesis of 1,4-Dihydroquinolines and Pyrrolo[1,2-a]quinolines via Intermolecular [4+2]/[3+2] Radical Cyclization of N-Methylanilines with Alkynoates
Sign Up to like & getrecommendations! Published in 2020 at "Synthesis"
DOI: 10.1055/s-0039-1691541
Abstract: Intermolecular [4+2]/[3+2] radical annulation of N-methylanilines with alkynoates under metal- and photoredox-catalyst-free conditions provides a practical and efficient method to synthesize bioactive 1,4-dihydroquinolines and pyrrolo[1,2-a]quinolines in one pot in moderate to high overall yields. read more here.
Keywords: intermolecular radical; free synthesis; dihydroquinolines pyrrolo; pyrrolo quinolines ... See more keywords