Enantioselective α-Arylation of Ketones via a Novel Cu(I)-Bis(phosphine) Dioxide Catalytic System
A novel catalytic system based on copper(I) and chiral bis(phosphine) dioxides is described. This allows the arylation of silyl enol ethers to access enolizable α-arylated ketones in good yields and enantiomeric excess up to 95%. Noncyclic ketones are amenable substrates with this method, which complements other approaches based on palladium catalysis. Optimization of the ligand structure is accomplished via rational design driven by correlation analysis. Preliminary mechanistic hypotheses are also evaluated in order to identify the role of chiral bis(phosphine) dioxides.
Escudero-Casao, Margarita,Licini, Giulia,Orlandi, Manuel
supporting information
p. 3289 - 3294
(2021/04/07)
Nickel-Catalyzed Cross-Coupling of Functionalized Organo manganese Reagents with Aryl and Heteroaryl Halides Promoted by 4-Fluorostyrene
A catalytic system consisting of Ni(acac) 2 (5 mol%) and 4-fluorostyrene (20 mol%) allows a convenient cross-coupling of functionalized organomanganese reagents with a variety of aryl and heteroaryl halides leading to polyfunctionalized diaryl- and arylheteroarylmethane derivatives.
Benischke, Andreas D.,Desaintjean, Alexandre,Juli, Thomas,Cahiez, Gérard,Knochel, Paul
supporting information
p. 5396 - 5412
(2017/12/14)
Identification of CKD-516: A potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors
Tubulin polymerization inhibitors had emerged as one of promising anticancer therapeutics because of their dual mechanism of action, i.e. apoptosis by cell-cycle arrest and VDA, vascular disrupting agent. VDAs are believed to be more efficient, less toxic
Lee, Jaekwang,Kim, Soo Jin,Choi, Hojin,Kim, Young Hoon,Lim, In Taek,Yang, Hyun-Mo,Lee, Chang Sik,Kang, Hee Ryong,Ahn, Soon Kil,Moon, Seung Kee,Kim, Dal-Hyun,Lee, Sungsook,Choi, Nam Song,Lee, Kyung Joo
experimental part
p. 6337 - 6354
(2010/10/21)
Weinreb amide based building blocks for convenient access to analogues of phenstatin
Bifunctional synthetic equivalents containing a Weinreb amide as one of the functionalities have been synthesized from commercially available o-, m-, and p-toluic acid. These bifunctional building blocks enabled efficient C-C bond formation through Wittig reaction with simple and functionalized aldehydes on one hand and a clean nucleophilic addition of 3,4,5-trimethoxy phenylmagnesium bromide onto the Weinreb amide functionality on the other hand, therebypaving way for an efficient and convenient synthesis of novel analogues of phenstatin with highly functionalized appendages. Further addition of various aryl or heteroarylmagnesium bromides onto theWeinreb amide functionality provided a general strategy for synthesizing unsymmetrical diaryl ketones conjugated to a monosaccharide moiety for the first time.
Sivaraman, Balasubramaniam,Aidhen, Indrapal Singh
experimental part
p. 4991 - 5003
(2010/11/05)
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