65321-30-4Relevant articles and documents
Weak base-promoted selective rearrangement of oxaziridines to amidesviavisible-light photoredox catalysis
Park, Jin,Park, Sehoon,Jang, Gwang Seok,Kim, Ran Hui,Jung, Jaehoon,Woo, Sang Kook
, p. 9995 - 9998 (2021/10/06)
The selective rearrangement of oxaziridines to amidesviaa single electron transfer (SET) pathway is unexplored. In this study, we present a weak base-promoted selective rearrangement of oxaziridines to amidesviavisible-light photoredox catalysis. The developed method shows excellent functional group tolerance with a broad substrate scope and good to excellent yields. Furthermore, control experiments and density functional theory (DFT) calculations are performed to gain insight into the reactivity and selectivity.
Catalyst-free synthesis of phenanthridinesviaelectrochemical coupling of 2-isocyanobiphenyls and amines
Malviya, Bhanwar Kumar,Singh, Karandeep,Jaiswal, Pradeep K.,Karnatak, Manvika,Verma, Ved Prakash,Badsara, Satpal Singh,Sharma, Siddharth
, p. 6367 - 6378 (2021/04/16)
Catalyst free synthesis of 6-aryl phenanthridines and amides through an electrochemical reaction is reported in this study. The coupling reaction proceeds by the cathodic reduction ofin situformed diazonium ions, which are formed from anilines and an alkyl nitrite. The generated aryl radical diazonium ions coupled from isocyanides furnished the desired products in good yields. This cascade reaction was conducted in an undivided cell equipped with an RVC as the anode and Pt as the cathode usingnBu4NBF4as the electrolyte at room temperature. A series of detailed mechanistic studies have also been performed, including a radical clock experiment and cyclic voltammetry analysis.
Highly efficient synthesis of amides via Ritter chemistry with ionic liquids
Kalkhambkar, Rajesh G.,Waters, Sarah N.,Laali, Kenneth K.
supporting information; experimental part, p. 867 - 871 (2011/03/18)
The utility of Br?nsted-acidic imidazolium ionic liquid [BMIM(SO3H)][OTf] as catalyst for the high yield synthesis of a wide variety of amides under mild conditions via the Ritter reaction of alcohols with nitriles has been demonstrated. As alternative methods for the carbocation generation step, NOPF6 immobilized in [BMIM][PF6] ionic liquid was used in the Ritter reaction of bromides with nitriles and for the synthesis of adamantyl amides from adamantane and nitriles.
Identification of orally available naphthyridine protein kinase D inhibitors
Meredith, Erik L.,Ardayfio, Ophelia,Beattie, Kimberly,Dobler, Markus R.,Enyedy, Istvan,Gaul, Christoph,Hosagrahara, Vinayak,Jewell, Charles,Koch, Keith,Lee, Wendy,Lehmann, HansJoerg,Mckinsey, Timothy A.,Miranda, Karl,Pagratis, Nikos,Pancost, Margaret,Patnaik, Anup,Phan, Dillon,Plato, Craig,Qian, Ming,Rajaraman, Vasumathy,Rao, Chang,Rozhitskaya, Olga,Ruppen, Thomas,Shi, Jie,Siska, Sarah J.,Springer, Clayton,Van Eis, Maurice,Vega, Richard B.,Von Matt, Anette,Yang, Lihua,Yoon, Taeyoung,Zhang, Ji-Hu,Zhu, Na,Monovich, Lauren G.
experimental part, p. 5400 - 5421 (2010/11/18)
A novel 2,6-naphthyridine was identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor. PKD inhibition in the heart was proposed as a potential antihypertrophic mechanism with application as a heart failure therapy. As PKC was previously identified as the immediate upstream activator of PKD, PKD vs PKC selectivity was essential to understand the effect of PKD inhibition in models of cardiac hypertrophy and heart failure. The present study describes the modification of the HTS hit to a series of prototype pan-PKD inhibitors with routine 1000-fold PKD vs PKC selectivity. Example compounds inhibited PKD activity in vitro, in cells, and in vivo following oral administration. Their effects on heart morphology and function are discussed herein.
[2, 6] NAPHTHYRIDINES USEFUL AS PROTEIN KINASE INHIBITORS
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Page/Page column 50, (2008/12/04)
The present invention provides a compound of formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.
Amide derivative
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, (2008/06/13)
A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1is hydogen atom, optionally substituted alkyl, etc.; R2and R3are independently optionally substituted alkyl, etc.; R4and R5are independently hydrogen atom or optionally substituted alkyl; R6is hydrogen atom, hydroxy or alkyl; or a pharmaceutically acceptable salt thereof is useful as a medicament for treating retinal degenerative disorders and the like.
Reaction of magnesiated bases on substituted pyridines: Deprotonation or 1,4-addition?
Bonnet, Veronique,Mongin, Florence,Trecourt, Francois,Queguiner, Guy
, p. 4245 - 4249 (2007/10/03)
N-(tert-Butyl)pyridine-2-carboxamide (1), N-phenylpyridine-2-carboxamide (7) and 2,2-dimethyl-N-(2-pyridyl)-propanamide (18) are readily deprotonated at C3 with a stoichiometric amount of PriMgCl or Bu2Mg in THF under reflux. Subsequ