434934-81-3Relevant academic research and scientific papers
Diazepinone derivatives
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Paragraph 0686-0687, (2014/03/24)
The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
DIAZEPINONE DERIVATIVES USEFUL FOR THE TREATMENT OF FRAGILE X SYNDROME, PARKINSONS OR REFLUX DISEASE
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Page/Page column 66, (2014/03/25)
The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
Approach to the synthesis of indoline derivatives from diaryliodonium salts
Landge, Kamalkishor P.,Jang, Keun Sam,Lee, Sang Yeul,Chi, Dae Yoon
experimental part, p. 5705 - 5713 (2012/09/07)
An effective method of constructing the indoline moiety via intramolecular nucleophilic ring closure of a diaryliodonium salt is described. Diacetoxyiodoarene compounds (1a-1e) were converted into intermediate Koser's reagent and coupled with arylstannanes (7-10) to form diaryliodonium salts (11a-14e). Indoline compounds with different N-protecting groups, 15, 16, 17, and 18, were synthesized in higher yields by treating salts (11a-14e) with Cs2CO3 and TEMPO. Regardless of the electronic environment of five para-substituted iodoarenes and the natures of four N-protected arylstannane groups, the conversion proceeded well to afford corresponding indolines in yields of 72-84 and 70-84%, respectively.
A mild inter- and intramolecular amination of aryl halides with a combination of CuI and CsOAc
Kubo, Tetsuji,Katoh, Chiharu,Yamada, Ken,Okano, Kentaro,Tokuyama, Hidetoshi,Fukuyama, Tohru
supporting information; experimental part, p. 11230 - 11236 (2009/04/11)
A unique combination of CuI and CsOAc was found to catalyze aryl amination under mild conditions. The reaction takes place at room temperature or at 90 °C with broad functional group compatibility. The intramolecular reaction was able to form five-, six-, and seven-membered rings with various protecting groups on the nitrogen atom. The scope of the intermolecular amination, as well as its applications to unsymmetrical N,N′-dialkylated phenylenediamines, was investigated.
Synthesis of indolines and tetrahydroisoquinolines from arylethylamines by PdII-catalyzed C-H activation reactions
Li, Jiao-Jie,Mei, Tian-Sheng,Yu, Jin-Quan
scheme or table, p. 6452 - 6455 (2009/03/11)
(Chemical Equation Presented) Hand in hand: A versatile C-H activation route for the synthesis of indolines, tetrahydroquinolines, and tetrahydroisoquinolines from simple arylethylamines relies on a one-pot iodination and amination reaction (see scheme, Tf=trifluoromethanesulfonyl). The natural amino acids phenylalanine, tyrosine, and tryptophan can be converted into various heterocycles by using this technology.
