35779-40-9Relevant academic research and scientific papers
Sequentially Pd/Cu-Catalyzed Alkynylation-Oxidation Synthesis of 1,2-Diketones and Consecutive One-Pot Generation of Quinoxalines
Niesobski, Patrik,Martínez, Ivette Santana,Kustosz, Sebastian,Müller, Thomas J. J.
supporting information, p. 5214 - 5218 (2019/07/31)
We report a simple and efficient one-pot synthesis of 1,2-diketones by concatenation of two Pd/Cu-catalyzed processes: Pd0/CuI-catalyzed Sonogashira coupling of terminal alkynes with aryl (pseudo)halides furnishes internal alkynes, which are directly transformed by PdII/CuII-catalyzed Wacker-type oxidation with DMSO and oxygen as dual oxidants to furnish 1,2-diketones. With this efficient, catalyst economical process, various aryl iodides and triflates are efficiently transformed in high yields into symmetrically and unsymmetrically substituted 1,2-diketones with various functional groups. This process can be readily extended to a consecutive one-pot synthesis of quinoxalines in a diversity-oriented fashion.
Diversity-Oriented Synthesis of a Library of Star-Shaped 2H-Imidazolines
Yu, Xuepu,Guttenberger, Nikolaus,Fuchs, Elisabeth,Peters, Martin,Weber, Hansj?rg,Breinbauer, Rolf
, p. 682 - 690 (2015/11/17)
A library of star-shaped 2H-imidazolines has been synthesized via Debus-Radziszewski condensation from 1,2-diketones and ketone starting materials. Selective reduction of one imine group of the 2H-imidazole intermediate with LiAlH4 or catalytic flow hydrogenation furnished 2H-imidazolines, which could be conveniently diversified by reacting the amine N with electrophiles, resulting in a set of 21 amide-, carbamate-, urea-, and allylamine-containing products. In total, five points of diversification could be used, which allow the production of a set of functionally diverse compounds. The synthesis of acylated 2H-imidazolidines resulted in intrinsically labile compounds, which spontaneously degraded to acyclic derivatives, as shown for the reaction of 2H-imidazolidine with hexylisocyanate.
Facile preparation of 1,2-diketones
Nowak, Pawel,Malwitz, David,Cole, Derek C.
experimental part, p. 2164 - 2171 (2010/08/13)
Easily accessible lead-like libraries of heterocyclic molecules useful for high-throughput screening are of continuous interest to the pharmaceutical industry. A number of drug-like libraries are derived from aromatic 1,2-diketones; however, nonsymmetrical 1,2-diketones are challenging to prepare. This communication describes a simple and practical synthesis of 1,2-diketones based on a controlled cross benzoin-like condensation reaction. Copyright Taylor & Francis Group, LLC.
Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
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Page/Page column 14-15, (2008/06/13)
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles
PYRAZINE DERIVATIVES USEFUL AS ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 57, (2008/06/13)
The present invention provides a compound of formula (I) wherein: A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group B represents an optionally substituted monocyclic nitrogen-containing heteroaryl group ; and either a) R1 and R2 represent hydrogen or specified substituents, or b) R2, R1 and the -NH- group to which R1 is attached, form a moiety selected from the moiety of formulae (IIa) and (IIb): (IIa) These compounds are useful as antagonists of the A2B receptor, for instance in the treatment of asthma.
OXIDATION OF SUBSTITUTED PYRIDINES PyrCH2X (X=H, COOR, COC6H5) WITH HYPERVALENT IODINE REAGENTS
Andrews, Ian P.,Lewis, Norman J.,McKillop, Alexander,Wells, Andrew S.
, p. 713 - 718 (2007/10/02)
Oxidation of a variety of pyridines, PyrCH2X (X=H, COOR, COC6H5) with hypervalent iodine reagents PhI(X)(Y) (X=OH, Y=OTs; X=Y=CH3COO; X=Y=CF3COO) has been studied.Simple alkylpyridines are unaffected by the reagents, but 2- and 4-substituted derivatives PyrCH2X (X=COOR, COC6H5) are oxidised at the CH2 group.
