5382-46-7Relevant academic research and scientific papers
Expedient carbonylation of aryl halides in aqueous or neat condition
Ang, Wei Jie,Lo, Lee-Chiang,Lam, Yulin
, p. 8545 - 8558 (2014/12/11)
An expedient and versatile, microwave-assisted procedure for the carbonylation of aryl halides with boronic acids, alcohols or amines in water or under neat conditions has been developed. The reaction is catalyzed by fluorous, oxime-based palladacycle 1 that shows an excellent recyclable property and low levels of Pd leaching. To demonstrate the usefulness of the protocol, we applied it to the preparation of compounds of pharmaceutical interest, including a precursor of the reverse transcriptase inhibitor, niacin, benzocaine and butamben.
Iron pentacarbonyl in alkoxy- and aminocarbonylation of aromatic halides
Babjak, Matej,Caletková, O?ga,?uri?ová, Diana,Gracza, Tibor
supporting information, p. 2579 - 2584 (2015/01/09)
We have identified reaction conditions for a Heck-type carbonylation based on [Fe(CO)5]. Preliminary optimization of alkoxycarbonylation on 2-bromonaphthalene defined functioning composition of the reaction mixture which was then applied on a small set of (hetero)aromatic halides. Respective aminocarbonylation of these halides with different amines, including aniline and benzotriazole, was accomplished with reasonable results.
Palladium-catalyzed fluorocarbonylation using N-formylsaccharin as CO source: General access to carboxylic acid derivatives
Ueda, Tsuyoshi,Konishi, Hideyuki,Manabe, Kei
supporting information, p. 5370 - 5373 (2013/11/06)
N-Formylsaccharin, an easily accessible crystalline compound, has been employed as an efficient CO source in Pd-catalyzed fluorocarbonylation of aryl halides to afford the corresponding acyl fluorides in high yields. The reactions use a near-stoichiometric amount of the CO source (1.2 equiv) and tolerate diverse functional groups. The acyl fluorides obtained could be readily transformed into various carboxylic acid derivatives such as carboxylic acid, esters, thioesters, and amides in a one-pot procedure.
N-Phenyl-4-hydroxy-2-quinolone-3-carboxamides as selective inhibitors of mutant H1047R phosphoinositide-3-kinase (PI3Kα)
Sabbah, Dima A.,Simms, Neka A.,Wang, Wang,Dong, Yuxiang,Ezell, Edward L.,Brattain, Michael G.,Vennerstrom, Jonathan L.,Zhong, Haizhen A.
, p. 7175 - 7183 (2013/01/15)
This work describes our efforts to optimize the lead PI3Kα inhibitor N-benzyl 4-hydroxy-2-quinolone-3-carboxamide using structure-based design and molecular docking. We identified a series of N-phenyl 4-hydroxy-2-quinolone-3- carboxamides as selective inhibitors of mutant H1047R versus wild-type PI3Kα and we also showed that the cell growth inhibition by these compounds likely occurs by inhibiting the formation of pAKT and induction of apoptosis.
