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Shamshin, V. P.; Aleshina, V. A.; Sukhanova, S. A.; Kabanova, T. I.

doi:10.1023/a:1012735616975

Cited by 2 publications

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“…The crude material was purified by column chromatography. Analytical data was found to match literature data: 4 a ,31 4 b ,5 4 c ,32 4 d ,33 4 e ,34 4 f ,35 4 h ,36 4 i ,37 4 j ,38 4 l ,39 and 4 m ,40.…”

Section: Methodssupporting

confidence: 73%

The Mg‐Oppenauer Oxidation as a Mild Method for the Synthesis of Aryl and Metallocenyl Ketones

Kloetzing

Krasovskiy

Knöchel

2006

Chemistry A European J

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Magnesium alkoxides undergo a hydride‐transfer oxidation with benzaldehyde as the oxidant. This magnesium variant of the Oppenauer oxidation was used for the synthesis of polyfunctional biaryl ketones. LiCl was found to promote this reaction by enhancing the solubility of magnesium alkoxides. This mild oxidation method was especially useful for preparing ketones bearing a metallocenyl unit as well as various new ferrocenyl ketones and tricarbonylchromium complexes. This last class of ketones was reduced with the CBS catalyst (CBS=Corey–Bakshi–Shibata, diphenyl oxazaborolidine) to chiral benzhydrol complexes with high enantioselectivity enabling an asymmetric synthesis of electron‐rich or ‐poor benzhydryl alcohols (up to 94 % ee).

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Section: Methodssupporting

confidence: 73%

The Mg‐Oppenauer Oxidation as a Mild Method for the Synthesis of Aryl and Metallocenyl Ketones

Kloetzing

Krasovskiy

Knöchel

2006

Chemistry A European J

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Synthesis and Evaluation of 3,4‐Dihydropyrimidin‐2(1H)‐ones as Sodium Iodide Symporter Inhibitors

2012

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The sodium iodide symporter (NIS) is responsible for the accumulation of iodide in the thyroid gland. This transport process is involved in numerous thyroid dysfunctions and is the basis for human contamination in the case of exposure to radioactive iodine species. 4-Aryl-3,4-dihydropyrimidin-2(1H)-ones were recently discovered by high-throughput screening as the first NIS inhibitors. Described herein are the synthesis and evaluation of 115 derivatives with structural modifications at five key positions on the pyrimidone core. This study provides extensive structure-activity relationships for this new class of inhibitors that will serve as a basis for further development of compounds with in vivo efficacy and adequate pharmacokinetic properties. In addition, the SAR investigation provided a more potent compound, which exhibits an IC(50) value of 3.2 nM in a rat thyroid cell line (FRTL5).

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Cited by 2 publications

References 1 publication

The Mg‐Oppenauer Oxidation as a Mild Method for the Synthesis of Aryl and Metallocenyl Ketones

The Mg‐Oppenauer Oxidation as a Mild Method for the Synthesis of Aryl and Metallocenyl Ketones

Synthesis and Evaluation of 3,4‐Dihydropyrimidin‐2(1H)‐ones as Sodium Iodide Symporter Inhibitors

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