1035217-13-0Relevant academic research and scientific papers
Nucleophilic Amination and Etherification of Aryl Alkyl Thioethers
Wang, Xia,Tang, Yue,Long, Cheng-Yu,Dong, Wen-Ke,Li, Chenchen,Xu, Xinhua,Zhao, Wanxiang,Wang, Xue-Qiang
supporting information, p. 4749 - 4753 (2018/08/23)
A transition-metal-free protocol capable of synthesizing diarylated aniline derivatives is reported. This method could be further employed to prepare aryl alkyl ethers. A wide range of thioethers, anilines, as well as alcohols were tolerated thanks to the mild reaction conditions. The strength of our method was demonstrated by performing a gram-scale reaction (20 mmol) followed by conversion of the nitrile group into synthetically useful aldehyde, ketone, and carboxylic acid.
Metal-Free Etherification of Aryl Methyl Ether Derivatives by C-OMe Bond Cleavage
Wang, Xueqiang,Li, Chenchen,Wang, Xia,Wang, Qingli,Dong, Xiu-Qin,Duan, Abing,Zhao, Wanxiang
supporting information, p. 4267 - 4272 (2018/07/29)
A general and efficient protocol was developed for the synthesis of aryl alkyl ethers through metal-free C-OMe bond cleavage under mild reaction conditions. This process displays a wide scope of methoxyarenes and alcohols, including primary, secondary, and tertiary alcohols, as well as natural products, pharmaceuticals, and biologically active alcohols. DFT calculations and experimental results simultaneously confirm that a potassium ion plays a critical role in the activation of methoxy group via binding with the nitrile and provide support for an SNAr mechanism.
(7-Benzyloxy-2,3-dihydro- 1H -pyrrolo[1,2-a]indol-1-yl)acetic acids as S1P1 functional antagonists
Buzard, Daniel J.,Lopez, Luis,Moody, Jeanne,Kawasaki, Andrew,Schrader, Thomas O.,Kasem, Michelle,Johnson, Ben,Zhu, Xiuwen,Thoresen, Lars,Kim, Sun Hee,Gharbaoui, Tawfik,Sengupta, Dipanjan,Calvano, Lorene,Krishnan, Ashwin,Gao, Yinghong,Semple, Graeme,Edwards, Jeff,Barden, Jeremy,Morgan, Michael,Usmani, Khawja,Chen, Chuan,Sadeque, Abu,Chen, Weichao,Christopher, Ronald J.,Thatte, Jayant,Fu, Lixia,Solomon, Michelle,Whelan, Kevin,Al-Shamma, Hussien,Gatlin, Joel,Gaidarov, Ibragim,Anthony, Todd,Le, Minh,Unett, David J.,Stirn, Scott,Blackburn, Anthony,Behan, Dominic P.,Jones, Robert M.
supporting information, p. 1334 - 1339 (2015/02/02)
S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery and optimization of (7-benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acids as potent, centrally available, direct acting S1P1 functional antagonists, with favorable pharmacokinetic and safety properties.
NOVEL BRONCHODILATING DIAZAHETEROARYLS
-
Page/Page column 34-35, (2012/03/08)
The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
NOVEL OXADIAZOLE COMPOUNDS
-
Page/Page column 138, (2011/06/26)
Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation o
PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF
-
Page/Page column 111, (2011/10/03)
The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
COMPOUNDS AS AGONISTS OF S1P1 RECEPTORS
-
Page/Page column 31, (2011/11/12)
Compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by S1P1 receptors.
NOVEL BRONCHODILATING DIAZAHETEROARYLS
-
Page/Page column 78-79, (2010/09/17)
The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
NOVEL OXADIAZOLE COMPOUNDS
-
Page/Page column 110-111, (2008/12/06)
Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation o
