14714-50-2Relevant academic research and scientific papers
Controlled meta-Selective C-H Mono- And Di-Olefination of Mandelic Acid Derivatives
Muthuraja, Perumal,Usman, Rahamdil,Sajeev, Revathy,Gopinath, Purushothaman
supporting information, p. 6014 - 6018 (2021/08/03)
Mandelic acids represent a key structural motif present in many drug molecules. Herein, we report the controlled meta-selective mono- and diolefination of mandelic acids by the careful design of the substrate and oxidant. Furthermore, free meta-functional
Expedited Kilolab Development of AZD7624 Using Kulinkovich-de Meijere Cyclopropanation
Ashok, Mithun,Ashwini, D. j.,Leuser, Helena,Malapati, Ajaya K.,Parker, Jeremy S.,Rowley, Naomi A.,Steven, Alan,Timms, Lee,Tyler, Simon N. G.,Whitmarsh, Samuel
, p. 2351 - 2366 (2021/10/21)
AZD7624 is a small molecule compound developed for the treatment of chronic obstructive pulmonary disease. This study describes the lab development and kilolab manufacture of the drug substance. A small number of route options were evaluated using lab pro
Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands
Gaiser, Birgit I.,Danielsen, Mia,Marcher-R?rsted, Emil,R?pke J?rgensen, Kira,Wróbel, Tomasz M.,Frykman, Mikael,Johansson, Henrik,Br?uner-Osborne, Hans,Gloriam, David E.,Mathiesen, Jesper Mosolff,Sejer Pedersen, Daniel
, p. 7806 - 7839 (2019/09/07)
Herein, we report the development of bitopic ligands aimed at targeting the orthosteric binding site (OBS) and a metastable binding site (MBS) within the same receptor unit. Previous molecular dynamics studies on ligand binding to the β2-adrenergic receptor (β2AR) suggested that ligands pause at transient, less-conserved MBSs. We envisioned that MBSs can be regarded as allosteric binding sites and targeted by homobivalent bitopic ligands linking two identical pharmacophores. Such ligands were designed based on docking of the antagonist (S)-alprenolol into the OBS and an MBS and synthesized. Pharmacological characterization revealed ligands with similar potency and affinity, slightly increased β2/β1AR-selectivity, and/or substantially slower β2AR off-rates compared to (S)-alprenolol. Truncated bitopic ligands suggested the major contribution of the metastable pharmacophore to be a hydrophobic interaction with the β2AR, while the linkers alone decreased the potency of the orthosteric fragment. Altogether, the study underlines the potential of targeting MBSs for improving the pharmacological profiles of ligands.
4-(aminomethyl)chromane-3-ol preparation method
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Paragraph 0007, (2019/12/25)
The invention relates to a 4-(aminomethyl)chromane-3-ol preparation method. A purpose of the present invention is mainly to solve the technical problem that no suitable industrial synthesis method exists in the prior art. According to the present inventio
Novel organic compounds derivatives and organic light-emitting diode therewith
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Paragraph 0550-0556, (2018/05/03)
The present invention relates to an organic compound represented by the chemical formula (A) or (B) and to an organic light-emitting device comprising the same. In the chemical formulas (A) and (B), R_1 to R_14, L1, L2, Ar1 to Ar3, n and m are as described in detailed description of the invention. The first object of the present invention is to provide the organic compound having a specific structure capable of having high efficiency, low voltage and long life characteristics by using the compound in an electron transporting layer or a hole transporting layer in the organic light emitting device.COPYRIGHT KIPO 2018
NOVEL HETEROCYCLIC COMPOUNDS AND ORGANIC LIGHT-EMITTING DIODE INCLUDING THE SAME
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Paragraph 0285; 0286; 0287; 0288; 0289, (2018/01/05)
Disclosed are an organic heterocyclic compound represented by Chemical Formula A and an organic light-emitting diode comprising the same.
Novel heterocyclic compounds and organic light-emitting diode including the same
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Paragraph 0455-0461, (2016/10/10)
The present invention relates to a novel heterocyclic compound having long lifespan properties, low voltage driving properties, and excellent light emitting efficiency, and an organic light emitting device comprising the same and, more specifically, to an organic light emitting compound represented by any one selected from chemical formula A and chemical formula B, and an organic light emitting device comprising the same. In chemical formulas, each substituent of A1 to A4, Randprime;, Randprime;andprime;, X, Y, and Z, and n are the same as defined in the detailed description of the invention.COPYRIGHT KIPO 2016
Palladium-catalyzed three-component coupling reactions of 2-(cyanomethyl)phenol, aryl halides, and carbon monoxide
Murai, Masahito,Okamoto, Kazuhiro,Miki, Koji,Ohe, Kouichi
, p. 4432 - 4437 (2015/06/08)
Three-component coupling reactions of 2-(cyanomethyl)phenol, aryl halides, and carbon monoxide (CO) in orthogonal-tandem catalysis were investigated. In the reactions, 2-(cyanomethyl)phenyl esters, which are produced through Pd(PPh3)4-catalyzed alkoxycarbonylation of aryl halides with 2-(cyanomethyl)phenol, undergo cycloisomerization in situ catalyzed by Pd(PCy3)2 as a co-catalyst to give 3-acyl-2-aminobenzofurans. Palladium species with homoleptic tertiary phosphines, such as Pd(PPh3)4 and Pd(PCy3)2, can catalyze the mechanistically distinct reactions in an orthogonal-tandem manner without interference. By switching the base used in this reaction, 3-acyl-2-(N-acylamino)benzofurans were obtained as major products instead of 3-acyl-2-aminobenzofurans. Given that 2-(cyanomethyl)phenols can be synthesized from commercially available salicylic acid derivatives in two steps, the present method thus provides facile access to synthetically useful 3-acyl-2-aminobenzofurans.
Ionic liquid-induced conversion of methoxymethyl-protected alcohols into nitriles and iodides using [Hmim][NO3]
Noei, Jalil,Mirjafari, Arsalan
supporting information, p. 4424 - 4426 (2014/08/05)
This Letter reports a one-pot efficient conversion of methoxymethyl-ethers into their corresponding nitriles and iodides using the ionic liquid, 1-methyl-3H-imidazolium nitrate ([Hmim][NO3]) under microwave irradiation. A variety of products were prepared in high yields using this method.
Copper-assisted/copper-free synthesis of functionalized dibenzo[b,f]oxepins and their analogs via a one-pot tandem reaction
Wang, Yuqin,Chen, Yanhong,He, Qian,Xie, Yuyuan,Yang, Chunhao
, p. 296 - 308 (2013/03/28)
A simple, convenient, and efficient method for the formation of functionalized dibenzo[b,f]oxepins and their analogs bearing both electron-donating and electron-withdrawing groups has been developed via a one-pot cascade reaction. Most starting materials are commercially available 2-(2-hydroxyphenyl)acetonitriles and 2-haloarylaldehydes. The procedure makes use of Cs2CO3 as the base, and DMF as solvent under copper-assisted/copper-free conditions. The reaction has a comprehensive group tolerance for substrates. Most of the reactions were complete within 1 h in good-to-excellent yields, and the reaction temperatures were relatively low. The protocol could be scaled up to grams without lowering the yield. A reaction mechanism was also proposed. Copyright
