77434-53-8Relevant academic research and scientific papers
Reusable Co-nanoparticles for general and selectiveN-alkylation of amines and ammonia with alcohols
Beller, Matthias,Gawande, Manoj B.,Jagadeesh, Rajenahally V.,Kadam, Ravishankar G.,Li, Xinmin,Ma, Zhuang,Petr, Martin,Zbo?il, Radek,Zhou, Bei
, p. 111 - 117 (2022/01/06)
A general cobalt-catalyzedN-alkylation of amines with alcohols by borrowing hydrogen methodology to prepare different kinds of amines is reported. The optimal catalyst for this transformation is prepared by pyrolysis of a specific templated material, which is generatedin situby mixing cobalt salts, nitrogen ligands and colloidal silica, and subsequent removal of silica. Applying this novel Co-nanoparticle-based material, >100 primary, secondary, and tertiary amines includingN-methylamines and selected drug molecules were conveniently prepared starting from inexpensive and easily accessible alcohols and amines or ammonia.
Controllable synthesis of 2- And 3-aryl-benzomorpholines from 2-aminophenols and 4-vinylphenols
Dong, Kui,Jin, Xiao-Ling,Chen, Shihao,Wu, Li-Zhu,Liu, Qiang
supporting information, p. 7941 - 7944 (2020/08/14)
We present herein a method for the controllable synthesis of 3-aryl-benzomorpholine and 2-aryl-benzomorpholine cycloadducts via cross-coupling/annulation between electron-rich 2-aminophenols and 4-vinylphenols. Molecular oxygen was successfully used in the reaction as the terminal oxidant and the complete inversion of chemoselectivity was achieved by the adjustment of the solvents and bases at room temperature.
Design, Synthesis, and Biological Activity of New N -(Phenylmethyl)-benzoxazol-2-thiones as Macrophage Migration Inhibitory Factor (MIF) Antagonists: Efficacies in Experimental Pulmonary Hypertension
Le Hiress, Morane,Akagah, Bernardin,Bernadat, Guillaume,Tu, Ly,Thuillet, Rapha?l,Huertas, Alice,Phan, Carole,Fadel, Elie,Simonneau, Gérald,Humbert, Marc,Jalce, Ga?l,Guignabert, Christophe
, p. 2725 - 2736 (2018/04/23)
Macrophage migration inhibitory factor (MIF) is a key pleiotropic mediator and a promising therapeutic target in cancer as well as in several inflammatory and cardiovascular diseases including pulmonary arterial hypertension (PAH). Here, a novel series of N-(phenylmethyl)-benzoxazol-2-thiones 5-32 designed to target the MIF tautomerase active site was synthesized and evaluated for its effects on cell survival. Investigation of structure-activity relationship (SAR) particularly at the 5-position of the benzoxazole core led to the identification of 31 that potently inhibits cell survival in DU-145 prostate cancer cells and pulmonary endothelial cells derived from patients with idiopathic PAH (iPAH-ECs), two cell lines for which survival is MIF-dependent. Molecular docking studies helped to interpret initial SAR related to MIF tautomerase inhibition and propose preferred binding mode for 31 within the MIF tautomerase active site. Interestingly, daily treatment with 31 started 2 weeks after a subcutaneous monocrotaline injection regressed established pulmonary hypertension in rats.
Oxidative transformation of N-substituted 2-aminophenols to 2-substituted benzoxazoles catalyzed by polymer-incarcerated and carbon-stabilized platinum nanoclusters
Yoo, Woo-Jin,Yuan, Hao,Miyamura, Hiroyuki,Kobayashi, Shu
experimental part, p. 306 - 313 (2012/04/17)
The preparation of 2-substituted benzoxazoles was achieved through a sequential aerobic oxidation-enolization-oxidative cyclization reaction of N-substituted 2-aminophenols catalyzed by platinum nanoclusters supported on a polymer/carbon black composite material.
Anti-allergic or anti-inflammatory substituted (hetero)-aralkylamino-ortho-phenols
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, (2008/06/13)
Compounds of the general formula (I) or a pharmaceutically acceptable salt or solvate thereof;, wherein R1 is straight or branched C1-6alkyl, halo, nitro, cyano, hydroxy, or COR6 wherein R6 is straight or branch
