Photocatalytic Late-Stage C-H Functionalization.
Sign Up to like & getrecommendations! Published in 2023 at "Chemical reviews"
DOI: 10.1021/acs.chemrev.2c00478
Abstract: The emergence of modern photocatalysis, characterized by mildness and selectivity, has significantly spurred innovative late-stage C-H functionalization approaches that make use of low energy photons as a controllable energy source. Compared to traditional late-stage functionalization… read more here.
Keywords: photocatalytic late; late stage; stage functionalization; chemistry ... See more keywords
Late-Stage C-H Functionalization of Azines.
Sign Up to like & getrecommendations! Published in 2023 at "Chemical reviews"
DOI: 10.1021/acs.chemrev.2c00881
Abstract: Azines, such as pyridines, quinolines, pyrimidines, and pyridazines, are widespread components of pharmaceuticals. Their occurrence derives from a suite of physiochemical properties that match key criteria in drug design and is tunable by varying their… read more here.
Keywords: stage functionalization; functionalization; chemistry; functionalization azines ... See more keywords
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00616
Abstract: Bacterial fatty acid synthases are promising antibacterial targets against multidrug-resistant pathogens. Platensimycin (PTM) is a potent FabB/FabF inhibitor, while its poor pharmacokinetics hampers the clinical development. In this study, a focused library of PTM derivatives… read more here.
Keywords: late stage; functionalization platensimycin; antibacterial activity; stage functionalization ... See more keywords
Rhodium-Catalyzed Annulation of Vinylated Tyrosines with Internal Alkynes to Access Oxepine-Mounted Unnatural Tyrosines and Its Peptide Late Stage Functionalization.
Sign Up to like & getrecommendations! Published in 2022 at "Organic letters"
DOI: 10.1021/acs.orglett.2c02820
Abstract: A Rh(III)-catalyzed [5+2] annulation of vinyl tyrosines with symmetrical and unsymmetrical internal alkynes was achieved, furnishing a series of oxepine-mounted tyrosine-based unnatural amino acids. In addition, the chemical applicability of the developed strategy was exemplified… read more here.
Keywords: stage functionalization; catalyzed annulation; internal alkynes; late stage ... See more keywords
Micro-photo-flow reactor system for fused N-heteroaryl scaffold synthesis and late-stage functionalization of pyrazolopyridines.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc03713k
Abstract: Late-stage functionalization (LSF) of active pharmaceutical ingredients can provide a straightforward approach to efficient de novo design and synthesis of drug molecules for structural activity relationship studies (SARS). Herein, we have developed a visible-light-driven modular… read more here.
Keywords: late stage; stage functionalization; flow reactor; fused heteroaryl ... See more keywords
Heteroarylation of unactivated C–H bonds suitable for late-stage functionalization
Sign Up to like & getrecommendations! Published in 2022 at "Chemical Science"
DOI: 10.1039/d2sc04605a
Abstract: The late-stage introduction of diverse heterocycles onto complex small molecules enables efficient access to new medicinally relevant compounds. An attractive approach to such a transformation would utilize the ubiquitous aliphatic C–H bonds of a complex… read more here.
Keywords: late stage; stage functionalization; stage; heteroarylation unactivated ... See more keywords
Green procedure for highly efficient, rapid synthesis of imidazo[1,2-a]pyridine and its late stage functionalization
Sign Up to like & getrecommendations! Published in 2018 at "Synthetic Communications"
DOI: 10.1080/00397911.2018.1434893
Abstract: ABSTRACT We unfold a rapid synthetic protocol for the preparation of imidazo[1,2-a]pyridine in cyclohexane. This methodology includes several advantages like shorter reaction time, catalyst free, broader substrate scope, and good yields of the desired products.… read more here.
Keywords: late stage; imidazo pyridine; pyridine; stage functionalization ... See more keywords