329946-26-1Relevant articles and documents
Diversification of 6-bromo-2-substituted Pyridine Derivatives via Suzuki-Miyaura Cross-Coupling
Lambert, Abigail E.,Carrick, Jesse D.
, p. 1232 - 1239 (2018)
The functionalized pyridine ring is a ubiquitous moiety in numerous research areas including materials, natural products, as well as agrochemicals and is a strategic synthon for heteroaromatic synthetic method development. Pyridinyl ligand scaffolds are also frequently incorporated into the study of metal complexes for pharmaceutical applications or separation science. Convergent access to advanced synthons is critical to experimentally defining structure activity relationships and improvement of molecular performance in the aforementioned areas. The current work describes an efficient catalyst/ligand combination for accessing 2-acetyl- and 2-procarbonyl substituted pyridines via Suzuki-Miyaura cross-coupling with various organotrifluoroborates. Twenty examples are described with carbonyl and procarbonyl functional groups which afford subsequent access to diversified unsymmetric ketones. Substrate scope and limitation in addition to?a scale up experiment are reported.
LDHA ACTIVITY INHIBITORS
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Page/Page column 39; 40, (2018/12/13)
The invention provides compounds of formula (I), stereoisomers and pharmaceutically acceptable salts thereof: (I) wherein A1 to A4, R1 and RP are as defined herein. Such compounds are suitable for use in the treatment or prevention of diseases or conditions which are mediated by the activation of lactate dehydrogenase A (LDHA), for example cancer.
LDHA ACTIVITY INHIBITORS
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Page/Page column 44, (2018/12/13)
The invention provides compounds of formula (I), stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof: (I) wherein A1 to A6 and R1 to R4 are as defined herein. Such compounds are suit