65000-13-7Relevant academic research and scientific papers
An approach to C-N activation: Coupling of arenesulfonyl hydrazides and arenesulfonyl chlorides with: Tert -amines via a metal-, oxidant- and halogen-free anodic oxidation
Sheykhan,Khani,Abbasnia,Shaabanzadeh,Joafshan
, p. 5940 - 5948 (2017/12/26)
tert-Amines were harnessed to afford arenesulfonyl hydrazides and arenesulfonyl chlorides via a metal-, oxidant- and halogen-free electrochemical oxidative coupling in an undivided cell at RT. This environmentally benign approach afforded a wide spectrum of sulfonamides in satisfactory yields using cheap and renewable Pencil Graphite Electrodes (PGEs).
Synthesis and Reactivity of 18F-Labeled α,α-Difluoro-α-(aryloxy)acetic Acids
Khotavivattana, Tanatorn,Calderwood, Samuel,Verhoog, Stefan,Pfeifer, Lukas,Preshlock, Sean,Vasdev, Neil,Collier, Thomas L.,Gouverneur, Véronique
supporting information, p. 568 - 571 (2017/02/10)
In this work, we describe the 18F-labeling of α,α-difluoro-α-(aryloxy)acetic acid derivatives and demonstrate that these building blocks are amenable to post-18F-fluorination functionalization. Protodecarboxylation offers a new entry to 18F-difluoromethoxyarene, and the value of this approach is further demonstrated with coupling processes leading to representative 18F-labeled TRPV1 inhibitors and TRPV1 antagonists.
Ruthenium olefin metathesis catalysts containing six-membered sulfone and sulfonamide chelating rings
Szadkowska, Anna,Zukowska, Karolina,Pazio, Aleksandra E.,Wozniak, Krzysztof,Kadyrov, Renat,Grela, Karol
experimental part, p. 1130 - 1138 (2011/04/26)
The preparation and X-ray structure characterization of new olefin metathesis initiators containing sulfone- and sulfonamide-substituted benzylidene ligands are described. We observed that these catalysts exhibit Ru???O(SO)R interactions, forming six-memb
Investigation of the mechanism of C(sp3)-H bond cleavage in Pd(0)-catalyzed intramolecular alkane arylation adjacent to amides and sulfonamides
Rousseaux, Sophie,Gorelsky, Serge I.,Chung, Benjamin K. W.,Fagnou, Keith
supporting information; scheme or table, p. 10692 - 10705 (2010/11/05)
The reactivity of C(sp3)-H bonds adjacent to a nitrogen atom can be tuned to allow intramolecular alkane arylation under Pd(0) catalysis. Diminishing the Lewis basicity of the nitrogen lone pair is crucial for this catalytic activity. A range of N-methylamides and sulfonamides react exclusively at primary C(sp3)-H bonds to afford the products of alkane arylation in good yields. The isolation of a Pd(II) reaction intermediate has enabled an evaluation of the reaction mechanism with a focus on the role of the bases in the C(sp3)-H bond cleaving step. The results of these stoichiometric studies, together with kinetic isotope effect experiments, provide rare experimental support for a concerted metalation-deprotonation (CMD) transition state, which has previously been proposed in alkane C(sp3)-H arylation. Moreover, DFT calculations have uncovered the additional role of the pivalate additive as a promoter of phosphine dissociation from the Pd(II) intermediate, enabling the CMD transition state. Finally, kinetic studies were performed, revealing the reaction rate expression and its relationship with the concentration of pivalate.
AMINOQUINAZOLINES COMPOUNDS
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Page/Page column 88-89, (2008/06/13)
The present invention is concerned with compounds of formula (1), wherein R1, R2 and X are as defined in the description and claims. The compounds of the present invention are PTP-1B inhibitors and can be used as medicaments.
