2982-53-8Relevant academic research and scientific papers
PIII/PV=O Catalyzed Cascade Synthesis of N-Functionalized Azaheterocycles
Li, Gen,Luzung, Michael R.,Nykaza, Trevor V.,Radosevich, Alexander T.,Yang, Junyu
supporting information, p. 4505 - 4510 (2020/02/05)
An organocatalytic method for the modular synthesis of diverse N-aryl and N-alkyl azaheterocycles (indoles, oxindoles, benzimidazoles, and quinoxalinediones) is reported. The method employs a small-ring organophosphorus-based catalyst (1,2,2,3,4,4-hexamethylphosphetane P-oxide) and a hydrosilane reductant to drive the conversion of ortho-functionalized nitroarenes into azaheterocycles through sequential intermolecular reductive C?N cross coupling with boronic acids, followed by intramolecular cyclization. This method enables the rapid construction of azaheterocycles from readily available building blocks, including a regiospecific approach to N-substituted benzimidazoles and quinoxalinediones.
Caged Naloxone: Synthesis, Characterization, and Stability of 3- O -(4,5-Dimethoxy-2-nitrophenyl)carboxymethyl Naloxone (CNV-NLX)
Lewin, Anita H.,Fix, Scott E.,Zhong, Desong,Mayer, Louise D.,Burgess, Jason P.,Mascarella, S. Wayne,Reddy, P. Anantha,Seltzman, Herbert H.,Carroll, F. Ivy
, p. 563 - 567 (2018/03/27)
The photolabile analogue of the broad-spectrum opioid antagonist naloxone, 3-O-(4,5-dimethoxy-2-nitrophenyl)carboxymethyl naloxone (also referred to as "caged naloxone", 3-O-(α-carboxy-6-nitroveratryl)naloxone, CNV-NLX), has been found to be a valuable biochemical probe. While the synthesis of CNV-NLX is simple, its characterization is complicated by the fact that it is produced as a mixture of αR,5R,9R,13S,14S and αS,5R,9R,13S,14S diastereomers. Using long-range and heteronuclear NMR correlations, the 1H NMR and 13C NMR resonances of both diastereomers have been fully assigned, confirming the structures. Monitoring of solutions of CNV-NLX in saline buffer, in methanol, and in DMSO has shown CNV-NLX to be stable for over a week under fluorescent laboratory lights at room temperature. Exposure of such solutions to λ 365 nm from a hand-held UV lamp led to the formation of naloxone and CNV-related breakdown products.
1,2-disubstituted-6-oxo-3-phenyl-piperidine-3-carboxamides and combinatorial libraries thereof
-
, (2008/06/13)
The invention relates to combinatorial libraries containing two or more novel piperidine-3-carboxamide derivative compounds, methods of preparing the piperidine-3-carboxamide derivative compounds and piperidine-3-carboxamide derivative compounds bound to a resin
Amine derivatives, processes for producing them and a use of them as antiarrhythmic drugs
-
, (2008/06/13)
PCT No. PCT/JP95/01138 Sec. 371 Date May 27, 1997 Sec. 102(e) Date May 27, 1997 PCT Filed Jun. 7, 1995 PCT Pub. No. WO96/04231 PCT Pub. Date Feb. 15, 1996Novel amine derivatives of the following general formula (I): (wherein) A may denote -(CH2)-O-, -(CH2)2-O-, or -(CH2)2-NH-; B may denote -(CH2)2-; R1 may denote a hydrogen atom, a halogen atom, a nitro group, a 1-pyrrolyl group, an acetamido group, an amino group or a dimethylamino group; R2 may denote a hydrogen atom or a nitro group; R3 and R4 may denote a hydrogen atom; R8a and R8b which are the same may denote a chlorine atom or a methoxy group; R9 may denote a hydrogen atom or an amino group; R may denote a methyl group; and X may denote a methanesulfonamido group, a 1-imidazolyl group or a nitro group or a salts thereof are useful as antiarrhythmic drugs.
Synthesis and biological activity of KCB-328 and its analogues: Novel class III antiarrhythmic agents with little reverse frequency dependence
Kim, Dong-Ick,Kim, Hak-Yeop,Kwon, Lae-Sung,Park, Sung-Dae,Jeon, Gee-Ho,Jung, Kyung-Yun,Min, Jae-Ki,Nam, Woong-Hyun,Lee, Kiho,Chung, You-Sup,Tanabe, Shigeru,Kozono, Toshiro
, p. 85 - 90 (2007/10/03)
A series of 3,4-dimethoxyphenethylamine derivatives was prepared, and their prolongation effects on effective refractory period of contractile response (ERPc) and action potential duration (APD) in isolated guinea-pig papillary muscles at 1 Hz and 3 Hz were examined. SAR studies led to the identification of KCB-328 (51) which is a novel class III antiarrhythmic agent with little reverse frequency dependence.
Nitrobenzene "Caged" Compounds as Irreversible Photoreductants: A Rational Approach to Studying Photoinduced Intermolecular Electron-Transfer Reactions in Proteins
DiMagno, Theodore J.,Stowell, Michael H. B.,Chan, Sunney I.
, p. 13038 - 13047 (2007/10/02)
Nitrobenzene "caged" compounds are well-known for their use in delivering biologically active substrates to a reaction mixture after photoexcitation.We have discovered that they also behave as photoreductants from the triplet state after photoexcitation.T
