38957-48-1Relevant academic research and scientific papers
Nickel-Catalyzed Directed Cross-Electrophile Coupling of Phenolic Esters with Alkyl Bromides
Ding, Decai,Wang, chuan,Yang, feiyan
supporting information, p. 9203 - 9209 (2020/12/22)
Herein, we demonstrate the successful use of robust phenolic esters as an electrophilic acyl source in the reaction with diverse primary and secondary unactivated alkyl bromides. The cleavage of the relatively inert C-O bond is facilitated by the neighboring coordinating hydroxyl or sulfonamide moiety. By circumventing the use of pregenerated organometallics, this method allows efficient preparation of a variety of o-hydroxyl and tosyl-protected o-amino aryl ketones with high compatibility with a wide range of functionalities.
INHIBITORS OF OPLOPHORUS LUCIFERASE-DERIVED BIOLUMINESCENT COMPLEXES
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Paragraph 00175; 00177-00178; 00305; 00307-00308; 00317, (2019/12/25)
Compounds that may selectively inhibit Oplophorus luciferase-derived bioluminescent complexes, e.g., NanoBiT? bioluminescent complex, are disclosed as well as compositions and kits comprising the compounds, and methods of using the compounds. The compounds are of formula (I) wherein R1-R4 and p and q are as defined in the claims.
Cu(II)-mediated C-H amidation and amination of arenes: Exceptional compatibility with heterocycles
Shang, Ming,Sun, Shang-Zheng,Dai, Hui-Xiong,Yu, Jin-Quan
supporting information, p. 3354 - 3357 (2014/03/21)
A Cu(OAc)2-mediated C-H amidation and amination of arenes and heteroarenes has been developed using a readily removable directing group. A wide range of sulfonamides, amides, and anilines function as amine donors in this reaction. Heterocycles present in both reactants are tolerated, making this a broadly applicable method for the synthesis of a family of inhibitors including 2-benzamidobenzoic acids and N-phenylaminobenzoates.
1-(2′-Anilinyl)prop-2-yn-1-ol rearrangement for oxindole synthesis
Kothandaraman, Prasath,Koh, Bing Qin,Limpanuparb, Taweetham,Hirao, Hajime,Chan, Philip Wai Hong
supporting information, p. 1978 - 1985 (2013/03/14)
A synthetic method that relies on NIS (N-iodosuccinimide)-mediated cycloisomerization reactions of 1-(2′-anilinyl)prop-2-yn-1-ols to gem-3-(diiodomethyl)indolin-2-ones and 2-(iodomethylene)indolin-3-ones has been developed. The reactions were shown to be chemoselective, with secondary and tertiary alcoholic substrates exclusively giving the 3- and 2-oxindole products, respectively. In the case of the latter, the transformation features an unprecedented double 1,2-OH and 1,2-alkyl migration relay. Density functional theory (DFT) calculations based on proposed iodoaminocyclization species provide insight into this unique divergence in product selectivity. Copyright
Metal-free synthesis of 1H-indole-2-carbaldehydes by N-iodosuccinimide- mediated cyclization of 1-(2′-anilinyl)prop-2-yn-1-ols in water. A formal synthesis of (R)-calindol
Kothandaraman, Prasath,Lauw, Sherman Jun Liang,Chan, Philip Wai Hong
, p. 7471 - 7480 (2013/08/23)
A N-iodosuccinimide (NIS)-mediated method to prepare 1H-indole-2- carbaldehydes efficiently from cycloisomerization of 1-(2-aminophenyl)prop-2-yn- 1-ols is described. The reaction is operationally straightforward and accomplished in good to excellent yiel
Microwave-induced rapid access to aromatic and heteroaromatic sulfonamides under solvent-free conditions without using external base
Sharma, Ashwani Kumar,Das, Saibal Kumar
, p. 3807 - 3819 (2007/10/03)
Microwave-induced syntheses of sulfonamides, without using base under solvent-free conditions, have been developed. The process finds its utility because of its simple operational procedure and high yields. Moreover, the process is fast and accommodative to different substituents on aromatic as well as heteroaromatic rings rendering sulfonamides (28 examples).
Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel
Peukert, Stefan,Brendel, Joachim,Pirard, Bernard,Struebing, Carsten,Kleemann, Heinz-Werner,Boehme, Thomas,Hemmerle, Horst
, p. 2823 - 2827 (2007/10/03)
The search for novel, potent Kv1.5 blockers based on an anthranilic amide scaffold employing a pharmacophore-based virtual screening approach is described. The synthesis and structure-activity relationships (SAR) with respect to inhibition of the Kv1.5 ch
