5952-93-2Relevant academic research and scientific papers
HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS
-
Paragraph 0671-0672; 0673, (2018/06/12)
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
A general continuous flow method for palladium catalysed carbonylation reactions using single and multiple tube-in-tube gas-liquid microreactors
Gross, Ulrike,Koos, Peter,O'brien, Matthew,Polyzos, Anastasios,Ley, Steven V.
supporting information, p. 6418 - 6430 (2016/02/18)
A series of continuous flow chemistry processes that facilitate the palladium-catalysed carbonylation of aryl and vinyl iodides and aryl bromides with a range of alkoxy, hydroxy and amino nucleophiles is reported. Harnessing a semipermeable Teflon AF-2400 Tube-in-Tube assembly, these reactors permit the controlled transport of carbon monoxide into solution at elevated pressure to generate homogeneous flow streams, avoiding some potential issues associated with segmented flow gas-liquid reactors. As the volume of pressurised gas contained within the device is low, the hazards associated with this are potentially mitigated relative to comparable batch processes. We also show how the incorporation of a second in-line gas-flow reactor allows for the sequential introduction of two gases (carbon monoxide and a gaseous nucleophile) into the reaction stream. A Teflon AF-2400 Tube-in-Tube reactor facilitates the use of carbon monoxide in continuous-flow C-C bond forming reactions providing esters, amides, carboxylic acids, lactones and lactams. Two reactors can be used in series to permit the sequential addition of two reactive gases (CO and Me2NH) into the flow stream.
Teflon AF-2400 mediated gas-liquid contact in continuous flow methoxycarbonylations and in-line FTIR measurement of CO concentration
Koos, Peter,Gross, Ulrike,Polyzos, Anastasios,O'Brien, Matthew,Baxendale, Ian,Ley, Steven V.
supporting information; experimental part, p. 6903 - 6908 (2011/10/31)
We report on the development of a continuous flow process for the palladium catalysed methoxycarbonylation of aryl, heteroaromatic and vinyl iodides and an aryl bromide using a Teflon AF-2400 based Tube-in-Tube reactor to mediate the selective permeation of carbon monoxide into solution at elevated pressures. The low volume of pressurised gas within the reactor (5.6 mL) offers the potential for an enhanced safety profile compared to batch processes. We also present preliminary results for the use of in situ FTIR to measure solution concentrations of carbon monoxide and demonstrate the use of a second reactor to effect the removal of carbon monoxide from the flow stream.
RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
-
Page/Page column 54, (2011/04/14)
Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment
Process for preparing heterocycles
-
, (2008/06/13)
Process for the preparation of heterocycles by reacting 2-substituted acetals of malondialdehyde with a reactant selected from hydroxylamines and their salts, hydrazines and their salts, formamid, amidines and their salts, guanidines and their salts, aminoguanidines and their salts, nitroguanidine and their salts, O-alkyl-isoureas and their salts, O-cycloalkyl-isoureas and their salts, O-aralkyl-isoureas and their salts, O-aryl-isoureas and their salts, S-alkyl-isothioureas, S-cycloalkyl-isothioureas, S-aralkyl-isothioureas, S-arylisothioureas, S-alkyl-isothiouronium salts, S-cycloalkyl-isothiouronium salts, S-aralkyl-isothiouronium salts, S-aryl-isothiuronium salts, thiourea and urea.
Novel generation of azomethine imines from α-silylnitrosamines by 1,4- silatropic shift and their cycloaddition
Washizuka, Ken-Ichi,Nagai, Keiko,Minakata, Satoshi,Ryu, Ilhyong,Komatsu, Mitsuo
, p. 8849 - 8853 (2007/10/03)
Novel and facile generation of azomethine imines from α- silylnitrosamines and subsequent cycloaddition with dipolarophiles leading to a variety of pyrazole derivatives have been developed. The key to the reaction is a 1,4-silatropic shift caused by stron
Synthesis of Halosulfuron-methyl via Selective Chlorination at 3- and/or 5-Position of Pyrazole-4-carboxylates
Morimoto, Katsushi,Sato, Toshiaki,Yamamoto, Susumu,Takeuchi, Hiroshi
, p. 537 - 540 (2007/10/03)
Reactions of methyl pyrazole-4-carboxylates 4b-d with N-chlorosuccinimide under heating conditions without a solvent gave methyl 3,5-dichloro-1-methylpyrazole-4-carboxylate 4a in good yields. The reaction of 4a with sodium hydrosulfide led to a nucleophilic substitution on the 5-position regioselectively to afford methyl 3-chloro-1-methyl-5-mercaptopyrazole-4-carboxylate 6a, which was followed by oxidative chlorination and amination to obtain 3-chloro-1-methyl-5-sulfamoylpyrazole-4-carboxylate 2a. Finally, the reaction of 2a with phenyl 4,6-dimethoxypyrimidin-2-yl carbamate 7 provided methyl 3-chloro-5-(4,6-dimethoxypyrimidin-2-ylcarbamoylsulfamoyl)-1-methylpyrazole-4- carboxylate (halosulfuron-methyl) 1a promising herbicide in corn.
Synthesis of 5-Chloropyrazoles by Chlorodiazoniation with Sulfur Dioxide
Yamamoto, Susumu,Morimoto, Katsushi,Sato, Toshiaki
, p. 1545 - 1547 (2007/10/02)
A facile synthesis of 5-chloropyrazoles 4a-e from 5-aminopyrazoles 2a-e via diazotization followed by chlorodediazoniation is described.A new application of sulfur dioxide as a catalyst was demonstrated to be the best for the chlorodediazoniation of diazonium chlorides 3a-e.
