314773-77-8Relevant articles and documents
An efficient synthesis of ortho-N-Boc-arylmethyl ketone derivatives
Broutin, Pierre-Emmanuel,Hilty, Peter,Thomas, Andrew W.
, p. 6429 - 6432 (2003)
A new and efficient method for the preparation of ortho-N-Boc-arylmethyl ketone derivatives is reported. The reaction involves the intermediacy of a 4-methylene-3,1-benzoaxin-2-one moiety which smoothly converts to the target compounds under acidic conditions. The ortho-N-Boc-arylmethyl ketone derivatives can be formed in a one-pot reaction or alternatively the 4-methylene-3,1-benzoaxin-2-ones can be isolated and subsequently transformed into the desired products.
A Convenient Formal [4+2] Heterocylization Route to Bis(triflyl)tetrahydroquinolines
Lázaro-Milla, Carlos,Almendros, Pedro
supporting information, p. 13534 - 13538 (2021/08/13)
We report the sustainable and efficient synthesis of a new type of quinoline derivatives bearing one or two SO2CF3 groups. The protocol is metal-, catalyst- and irradiation-free, involves the use of readily available and stable precursors, and avoids the formation of side products. Also, the mild conditions of the process allow the tolerance of a wide range of functional groups.
Rational modification, synthesis and biological evaluation of 3,4-dihydroquinoxalin-2(1H)-one derivatives as potent and selective c-Jun N-terminal kinase 3 (JNK3) inhibitors
Dou, Xiaodong,Huang, Huixia,Jiang, Lan,Jiao, Ning,Jin, Hongwei,Liu, Zhenming,Zhang, Liangren,Zhang, Lihe,Zhu, Guiwang
, (2020/07/03)
The c-Jun N-terminal kinase 3 (JNK3) plays key roles in a wide range of diseases, including neurodegeneration diseases, inflammation diseases, cancers, cardiovascular diseases, and metabolic disorders. Previously, we have identified a lead compound, (Z)-3
Construction of 1H-indazoles from ortho-aminobenzoximes by the Mitsunobu reaction
Conlon, Ivie L.,Konsein, Katie,Morel, Yulemni,Chan, Alexandria,Fletcher, Steven
, (2019/08/22)
Recently, there has been an upsurge in the occurrence of the indazole motif in drug discovery. Accordingly, newer, milder and more efficient routes towards their synthesis have emerged in the literature. We recently reported the Mitsunobu-triggered cyclod
One pot synthesis of α-ketoamides from ethylarenes and amines: a metal free difunctionalization strategy
Ramanathan, Mani,Kuo, Chun-Kai,Liu, Shiuh-Tzung
, p. 11446 - 11453 (2016/12/16)
One-pot and metal free synthesis of α-ketoamides has been described through in situ generation of aryl ketones from easily available ethylarenes followed by amidation with various amines. This multiple oxidation protocol involves catalytic I2-pyridine-TBHP (t-butyl hydroperoxide) mediated oxidative benzylic carbonylation and sequential NaI-TBHP mediated oxidative amidation without using any solvent.
N-Heterocyclic Carbene-Catalyzed Synthesis of 2-Aryl Indoles
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Paragraph 0064-0065, (2015/11/27)
Transition metal-free catalytic methods for access to 2-arylindole compounds.
N-heterocyclic-carbene-catalyzed synthesis of 2-aryl indoles
Hovey, M. Todd,Check, Christopher T.,Sipher, Alexandra F.,Scheidt, Karl A.
supporting information, p. 9603 - 9607 (2014/10/15)
A convergent and efficient transition-metal-free catalytic synthesis of 2-aryl-indoles has been developed. The interception of a highly reactive and transient aza-ortho-quinone methide by an acyl anion equivalent generated through N-hetereocyclic carbene catalysis is central to this successful strategy. High yields and a wide scope as well as the streamlined synthesis of a kinase inhibitor are reported. Umpolung: N-heterocyclic carbene catalysis is used for the convergent and efficient transition-metal-free synthesis of 2-aryl-indoles. The interception of a highly reactive and transient aza-ortho-quinone methide by an acyl anion equivalent is central to this successful strategy. The reaction exhibits high yields and a wide scope, and it has been applied to a streamlined synthesis of a kinase inhibitor.
Enzymatic kinetic resolution of tert-butyl 2-(1-Hydroxyethyl) phenylcarbamate, a key intermediate to chiral organoselenanes and organotelluranes
Piovan, Leandro,Pasquini, Monica D.,Andrade, Leandro H.
experimental part, p. 8098 - 8109 (2011/11/06)
The enzymatic kinetic resolution of tert-butyl 2-(1-hydroxyethyl) phenylcarbamate via lipase-catalyzed transesterification reaction was studied. We investigated several reaction conditions and the carbamate was resolved by Candida antarctica lipase B (CAL
THIADIAZOLINE DERIVATIVES
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Page/Page column 40; 43, (2010/11/08)
An antitumor agent comprising a thiadiazoline derivative represented by the general formula (I), or a pharmacologically acceptable salt thereof as an active ingredient: (wherein Z represents a sulfur atom and the like, R1 represents substituted or unsubstituted lower alkynyl and the like, R2 represents a hydrogen atom and the like, R3 represents substituted or unsubstituted lower alkyl and the like, and R4 represents substituted or unsubstituted aryl and the like), and the like are provided.
THERAPEUTIC AGENT FOR RESTENOSIS
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Page/Page column 81-82, (2010/11/25)
A therapeutic and/or prophylactic agent for restenosis comprising a thiadiazoline derivative represented by the general formula (O) or a pharmaceutically acceptable salt thereof: wherein n represents an integer of 1 to 3; R0 represents an aryl,