54804-43-2Relevant academic research and scientific papers
Side chain bromination of mono and dimethyl heteroaromatic and aromatic compounds by solid phase N-bromosuccinimide reaction without radical initiator under microwave
Goswami, Shyamaprosad,Dey, Swapan,Jana, Subrata,Adak, Avijit Kumar
, p. 916 - 917 (2007/10/03)
A series of side chain mono and dibromo derivatives of mono and dimethyl heteroaromatic and aromatic compounds (1-17) were synthesized by one step solid phase N-bromosuccinimide (NBS) reaction without radical initiator by microwave irradiation. The benzylic mono and dibromo products were exclusively preferred except in the case of 6-methylpyridine amides (8 and 9) where nuclear and also side chain bromination resulted. Naphthyridine systems resulted improved yields. By this method, we also report the synthesis of 2-pivaloylaminopterin-6- carbaldehyde.
Method for preparing heterocyclic-carboxylic acids
-
, (2008/06/13)
The present invention relates to a method for preparing quinoxaline-5- and 6-carboxylic acids. The method comprises contacting an aqueous suspension of a 5- or 6-hydroxymethyl quinoxaline with oxygen in the presence of a transition metal catalyst, to form the respective quinoxaline-5- or 6-carboxylic acid. The method for oxidizing benzylic methyl groups may also be employed to prepare a wide variety of heterocyclic carboxylic acid compounds.
On the development of NAD(P)H-sensitive fluorescent probes
Maidwell, Nicola L.,Reza Rezai,Roeschlaub, Carl A.,Sammes, Peter G.
, p. 1541 - 1546 (2007/10/03)
In contrast to current, multi-reagent assay systems, the development of a single reagent that can be used to assay NAD(P)H is described. The reagent eliminates the fluorophore 4-methylumbelliferone from a quinoxalinium adduct upon reduction and the chemistry of this process is described. The Royal Society of Chemistry.
Synthesis and Selective Class III Antiarrhythmic Activity of Novel N-Heteroaralkyl-Substituted 1-(Aryloxy)-2-propanolamine and Related Propylamine Derivatives
Butera, John A.,Spinelli, Walter,Anantharaman, Viji,Marcopulos, Nicholas,Parsons, Roderick W.,et al.
, p. 3212 - 3228 (2007/10/02)
The synthesis and biological evaluation of a series of novel 1-(aryloxy)-2-propanolamines and several related deshydroxy analogues are described.Compounds 4-29 were prepared and investigated for their class III electrophysiological activity in isolated canine Purkinje fibers and in anesthetized open-chest dogs.None of these compounds showed any class I activity.On the basis of the in vitro data, structure-activity relationships for the series are discussed.Two compounds, N-propoxy>phenyl>methanesulfonamide (12, WAY-123,223) and N-phenoxy>propyl>amino>methyl>-6-quinolinyl>methanesulfonamide (24, WAY-125,971) were identified and characterized as potent and specific class III antiarrhythmic agents in vitro and in vivo.Compound 12 was found to be orally bioavailable, to produce large increases of ventricular fibrillation threshold (VFT), and, in some instances, to restore sinus rhythm from ventricular fibrillation in anesthetized open-chest dogs at a dose of 5 mg/kg (iv).The enantiomers of 12 (i.e., 13 and 14) were synthesized and were found to exhibit similar electrophysiological effects in the Purkinje fiber screen.Compound 24, a propylamine analogue with potency and efficacy comparable to those of UK-68798 (2) and E-4031 (3), was studied in voltage-clamp experiments (isolated cat myocytes) and was found to be a potent and specific blocker of the delayed rectifier potassium current (IK).
