A Study on the Quality Characteristics of Feedstocks for Power Bio-Fuel Oil

Profound Methyl Effects in Drug Discovery and a Call for New CH Methylation Reactions

“…Some key advancements in directed CÀH methylation with methyl iodide include a recent report from the Chen research group that details the use of O 2 as the sole oxidant (entry 1), [49] while Jang and Youn report conditions that allow the reaction to proceed in a reasonable amount of time at room temperature (entry 2). [50] Sanford and co-workers have recently developed a mild procedure that makes use of methyl trifluoroborate…”

Sulfonium Salts as Alkylating Agents for Palladium-Catalyzed Direct Ortho Alkylation of Anilides and Aromatic Ureas

“…We found that in polar solvents the reaction did not work, but less polar, non-protic solvents such as toluene, DCM, DCE were suitable for the transformation (Table 1, entries 1-7). Regarding the catalyst loading, the conversion of the reaction changed proportionally to the amount of palladium (entries [8][9]. Additionally, the presence of 5 equiv acid was found to be necessary for the complete suppression of the formation of N-alkylated byproduct.…”

“…6 Although, one of the earliest examples of C-H activation reactions described the direct alkylation of anilides using stoichiometric palladium, 7 the introduction of alkyl groups under catalytic conditions has remained a challenging task, especially under mild reaction conditions. 8 Existing alkylation methods often suffer from the loss of selectivity or byproduct formation, as chain isomerization in Friedel-Crafts or -H-elimination in transi-tion metal catalyzed coupling reactions. Additionally, to the best of our knowledge there is only one existing method for the ortho alkylation of aromatic ureas through direct C-H bond functionalization, considering both traditional and transition metal catalyzed methods.…”

Ausgeprägte Methyleffekte in der Wirkstoff‐Forschung und der Bedarf an neuen C‐H‐Methylierungsreaktionen

“…[47,48] Zu den wichtigen Fortschritten in der gerichteten C-H-Methylierung mit Methyliodid gehçren die kürzlich von Chen und Zhao beschriebene Verwendung von O 2 als einzigem Oxidationsmittel (Eintrag 1) [49] sowie die von Youn und Jang entwickelten Bedingungen, die eine Umsetzung bei Raumtemperatur in angemessener Zeit ermçglichen (Eintrag 2). [50] Sanford et al entwickelten vor kurzem eine milde Methode mit Trifluorborat und einer Manganverbindung als Aktivator (Eintrag 7). [51] Eine interessante praktische Anwendung dieser Chemie ist die von Yu et al in Zusammenarbeit mit Pfizer entwickelte Methylierung der fortgeschrittenen Zwischenstufe eines Analogons des Entzündungshemmers Celecoxib (Eintrag 8).…”