79903-04-1Relevant articles and documents
A B2(OH)4-Mediated Synthesis of 2-Substituted Indazolone and Its Application in a DNA-Encoded Library
Bao, Yapeng,Deng, Zongfa,Feng, Jing,Zhu, Weiwei,Li, Jin,Wan, Jinqiao,Liu, Guansai
supporting information, p. 6277 - 6282 (2020/08/24)
Indazolone cores are among the most common structural components in medicinal chemistry and can be found in many biologically active molecules. In this report, a mild and efficient approach to 2-substituted indazolones via B2(OH)4-mediated reductive N-N b
Aminocarbonylations employing Mo(CO)6 and a bridged two-vial system: Allowing the use of nitro group substituted aryl iodides and aryl bromides
Nordeman, Patrik,Odell, Luke R.,Larhed, Mats
, p. 11393 - 11398 (2013/02/23)
A bridged two-vial system aminocarbonylation protocol where Mo(CO) 6 functions as an external in situ solid source of CO has been developed. For the first time both nitro group containing aryl/heteroaryl iodides and bromides gave good to excellent yields in the Mo(CO) 6-mediated and palladium(0)-catalyzed conversion to benzamides, while the identical one-vessel protocol afforded extensive reduction of the nitro functionality. The above-mentioned bridged two-compartment protocol furnished good results with both primary amines and secondary amines and sluggish aniline nucleophiles at 65-85 C reaction temperatures.
QUINAZOLINONE AND FUSED PYRIMIDINONE COMPOUNDS AND THEIR USE IN TREATING SODIUM CHANNEL-MEDIATED DISEASES OR CONDITIONS
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Page/Page column 109, (2008/12/07)
This invention is directed to compounds of formula (I): wherein (A), n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
MECHANISM OF ESTER AMINOLYSIS IN APROTIC MEDIA AND SPECIFIC SOLVENT EFFECTS
Nagy, Otto B.,Reuliaux, Victor,Bertrand, Nicole,Mensbrugghe, Anne Van Der,Leseul, Jean,Nagy, Janos B.
, p. 1055 - 1074 (2007/10/02)
The n-butylaminolysis of nitro-substituted 4'-nitrophenyl benzoates and cinnamates as well as of phenylacetates in aprotic solvents is governed by a kinetic law implying higher order terms in nucleophile.It is shown that the attacking nucleophile forms a n-? type molecular complex with the substrate before reaching the transition state in the subsequent kinetic step.This molecular complex is a true reaction intermediate as evidenced by the observed negative activation enthalpy.Other nucleophile molecules intervene as general base catalysts.Tertiary amines also catalyse the reaction.Their catalytic activity is linearly related to their hydrogen bond forming ability and it is not a direct function of their proton basicity.By varying the nucleophile structure, an excellent Broensted relationship could be obtained for the first time in aprotic media, the β of which confirms that the catalytic collapse of tetrahedral intermediate is the rate determining step.The reaction of cinnamates turns out to be less sensitive to structural changes of the substrate than is the reaction of benzoates as shown by the corresponding Hammet ? values.The electronic effects of 2-nitro groups are strongly solvent dependent.Once more, it is established that whenever specific solvent effects (?-donor or n-donor ability) are present, they dominate the overall effect.A general reaction mechanism is proposed which not only explains the various roles played by the nucleophile but also accounts successfully for the great variety of kinetic schemes observed in aprotic media.
