19090-04-1Relevant articles and documents
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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, (2021/07/31)
Provided herein are novel heterocyclic compounds, for example, compounds having Formula I, I-P, II, lI-P, or III. Also provided herein are pharmaceutical compositions comprising the compounds and methods of using the same, for example, in inhibiting aldehyde dehydrogenases and/or for treating various cancers, cancer metastasis, type 2 diabetes, pulmonary arterial hypertension (PAH) or neointimal hyperplasia (NIH).
Carbonyl 1,2-transposition through triflate-mediated a-amination
Wu, Zhao,Xu, Xiaolong,Wang, Jianchun,Dong, Guangbin
, p. 734 - 740 (2021/11/16)
To date, it remains challenging to selectively migrate a carbonyl oxygen within a given molecular scaffold, especially to an adjacent carbon. In this work, we describe a simple one- or two-pot protocol that transposes a ketone to the vicinal carbon. This approach first converts the ketone to the corresponding alkenyl triflate, which can then undergo the palladium- and norbornene-catalyzed regioselective a-amination and ipso-hydrogenation enabled by a bifunctional hydrogen and nitrogen donor. The resulting "transposed enamine" intermediate can subsequently be hydrolyzed to produce the 1,2-carbonyl-migrated product. This method allows rapid access to unusual bioactive analogs through late-stage functionalization.
Rh-catalyzed intramolecular aromatic C-H insertion of α-diazo β-ketoesters: Synthesis of 4-carbonyl chroman derivatives
Zhang, Xiaolin,Lei, Mei,Zhang, Yi-Nan,Hu, Li-Hong
, p. 3400 - 3406 (2014/05/06)
A Rh-catalyzed intramolecular aromatic C-H insertion of α-diazo β-ketoesters was developed. This protocol offers a practical strategy for the synthesis of 4-carbonyl chroman derivatives with high yield and is compatible with a wide variety of substituents