446-47-9Relevant academic research and scientific papers
SUBSTITUTED BENZOTHIOPHENE ANALOGS AS SELECTIVE ESTROGEN RECEPTOR DEGRADERS
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Paragraph 0318, (2019/08/29)
In one aspect, the disclosure relates to relates to substituted benzothiophene analogs which are useful as selective degraders of estrogen receptor, methods of making same, pharmaceutical compositions comprising same, and methods of treating one or more clinical conditions associated with estrogen receptor, such as a cancer, including breast cancer, or osteoporosis. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Nucleophilic fluorination facilitated by a CsF-CaF2 packed bed reactor in continuous flow
Johansen,Lindhardt
supporting information, p. 825 - 828 (2018/02/06)
A simple to prepare, dry and handle packed bed reactor carrying CsF on CaF2, towards nucleophilic fluorinations in continuous flow, is reported. The reactor also proved adaptable for silyl-ether deprotection and trifluoromethylations with Ruppert's reagent. The study includes reactor stability and scale-up investigations.
Towards iron-catalysed suzuki biaryl cross-coupling: Unusual reactivity of 2-halobenzyl halides
Bedford, Robin B.,Gallagher, Timothy,Pye, Dominic R.,Savage, William
, p. 1761 - 1765 (2015/06/16)
The reaction of 2-halobenzyl halides with the borate anion Li[(Ph)(t-Bu)Bpin] leads not only to the expected arylation at the benzyl position, but also to some Suzuki biaryl cross-coupling. Preliminary mechanistic investigations hint towards the intermediacy of benzyl iron intermediates that can either: (a) directly cross-couple with the aryl boron reagent to give observed monoarylated species, or (b) undergo oxidative addition of the aryl halide to generate the diarylated species on reaction with the boron-based nucleophile.
Long-range bonding/nonbonding interactions: A donor-acceptor resonance studied by dynamic NMR
Ruzziconi, Renzo,Lepri, Susan,Buonerba, Federica,Schlosser, Manfred,Mancinelli, Michele,Ranieri, Silvia,Prati, Luca,Mazzanti, Andrea
supporting information, p. 2740 - 2743 (2015/06/16)
Long-range bonding interactions were evaluated using variable-temperature NMR spectroscopy and suitable 2′-CH2X-substituted phenylpyridines (X = Me, NMe2, OMe, F). It was found that the arylpyridyl rotational barriers were lower when electronegative atoms were bound to the α carbon of the 2′ moiety. This effect was ascribed to a stabilizing interaction in the transition state due to the lone pair of the heterocyclic nitrogen with the α carbon. Computational support for this hypothesis came from CCSD(T)/6-31+G(d) calculations. Steric effects of the X moiety were ruled out by comparison of the rotational barriers of analogous biphenyls.
Friedel-crafts reaction of benzyl fluorides: Selective activation of C-f bonds as enabled by hydrogen bonding
Champagne, Pier Alexandre,Benhassine, Yasmine,Desroches, Justine,Paquin, Jean-Franois
supporting information, p. 13835 - 13839 (2015/02/05)
A Friedel-Crafts benzylation of arenes with benzyl fluorides has been developed. The reaction produces 1,1-diaryl alkanes in good yield under mild conditions without the need for a transition metal or a strong Lewis acid. A mechanism involving activation of the C-F bond through hydrogen bonding is proposed. This mode of activation enables the selective reaction of benzylic C-F bonds in the presence of other benzylic leaving groups.
FLUORINATION OF HALOGENO ALCOHOLS WITH 1,1,2,3,3,3-HEXAFLUOROPROPYL DIETHYLAMINE
Watanabe, S.,Fujita, T.,Usui, Y.,Kimura, Y.
, p. 135 - 142 (2007/10/02)
Fluorination of halogeno alcohols with 1,1,2,3,3,3-hexafluoropropyl diethylamine (PPDA) was investigated. 2-Bromo-1-fluorobutane was obtained from the reaction of PPDA and 2-bromo-1-butanol (yield 50percent).Similar results were obtained from other alipha
