10224-71-2Relevant articles and documents
Selective sodium channel regulator as well as preparation and application thereof
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Paragraph 0401-0405, (2021/02/10)
The invention provides a compound serving as a selective sodium channel regulator and a synthesis and use method, and particularly provides a compound shown as a formula (I), a preparation method of the compound and application of the compound serving as the selective sodium channel regulator. The compounds exhibit excellent activity as a regulator of sodium channels.
Self-Immolative System for Disclosure of Reactive Electrophilic Alkylating Agents: Understanding the Role of the Reporter Group
Chippindale, Ann M.,Gavriel, Alexander G.,Hayes, Wayne,Khurana, Gurjeet S.,Leroux, Flavien,Lewis, Viliyana G.,Russell, Andrew T.,Sambrook, Mark R.
, p. 10263 - 10279 (2021/08/16)
The development of stable, efficient chemoselective self-immolative systems, for use in applications such as sensors, requires the optimization of the reactivity and degradation characteristics of the self-immolative unit. In this paper, we describe the effect that the structure of the reporter group has upon the self-immolative efficacy of a prototype system designed for the disclosure of electrophilic alkylating agents. The amine of the reporter group (a nitroaniline unit) was a constituent part of a carbamate that functioned as the self-immolative unit. The number and position of substituents on the nitroaniline unit were found to play a key role in the rate of self-immolative degradation and release of the reporter group. The position of the nitro substituent (meta- vs para-) and the methyl groups in the ortho-position relative to the carbamate exhibited an influence on the rate of elimination and stability of the self-immolative system. The ortho-methyl substituents imparted a twist on the N-C (aromatic) bond leading to increased resonance of the amine nitrogen's lone pair into the carbonyl moiety and a decrease of the leaving character of the carbamate group; concomitantly, this may also make it a less electron-withdrawing group and lead to less acidification of the eliminated β-hydrogen.
SELF-IMMOLATIVE SYSTEMS
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Page/Page column 10; 24-26, (2020/05/28)
The present invention is concerned with self-immolative recognition and/or responsive systems for electrophilic compounds, especially alkylating agents, which systems may comprise disclosure or detection of the alkylating agent. The present invention is especially concerned with non-protic triggered self-immolative systems, molecules, and methods, and in particular for detection of non- protic electrophilic agents, and especially alkylating agents, for example alkyl or benzylic halides, which may be found in pesticides or fumigants, or chemical warfare agents.
Palladium-catalyzed amidation by chemoselective C(sp3)-H activation: Concise route to oxindoles using a carbamoyl chloride precursor
Tsukano, Chihiro,Okuno, Masataka,Takemoto, Yoshiji
supporting information; experimental part, p. 2763 - 2766 (2012/05/05)
Quite select: A new strategy was developed for the synthesis of various oxindoles from carbamoyl chlorides. Under the optimum reaction conditions, with Ad2PBu as a ligand, tBuCONHOH as an additive, and a CO atmosphere, selective C(sp3/sup
2,4 DI (HETERO) -ARYLAMINO-PYRIMIDINE DERIVATIVES AS ZAP-70 AND/OR SYK INHIBITORS
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Page/Page column 33, (2010/02/11)
Disclosed are pyrimidine derivatives of formula (I); wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have ZAP-70 and/or Syk inhibitory activities.
Dyeing keratin fibers with 2-substituted m-toluenediamines
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, (2008/06/13)
Oxidation dye compositions particularly useful for dyeing human hair containing as the meta component compounds of the formula: STR1 or their non-toxic salts, wherein R is alkyl, hydroxyalkyl, phenylalkyl, phenylsulfonyls, alkylsulfonyls or cyanoalkyl.
