- Nickel-Catalyzed Reductive Cross-Coupling of Aryl Bromides with Vinyl Acetate in Dimethyl Isosorbide as a Sustainable Solvent
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A nickel-catalyzed reductive cross-coupling has been achieved using (hetero)aryl bromides and vinyl acetate as the coupling partners. This mild, applicable method provides a reliable access to a variety of vinyl arenes, heteroarenes, and benzoheterocycles, which should expand the chemical space of precursors to fine chemicals and polymers. Importantly, a sustainable solvent, dimethyl isosorbide, is used, making this protocol more attractive from the point of view of green chemistry.
- Su, Mincong,Huang, Xia,Lei, Chuanhu,Jin, Jian
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supporting information
p. 354 - 358
(2022/01/15)
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- FORMS AND COMPOSITIONS OF A BETA ADRENERGIC AGONIST
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The present disclosure relates generally to various forms and compositions useful as beta adrenergic agonists and uses of the same in the treatment of diseases associated with an adrenergic receptor. In one aspect, the disclosure provides a crystalline solid form of Compound 1: selected from Form A and Form B and salt forms thereof.
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Paragraph 00439
(2021/12/30)
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- BETA ADRENERGIC AGONIST AND METHODS OF USING THE SAME
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The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor. In certain embodiments of the methods disclosed herein, the methods include administering to the subject a compound as disclosed herein and a peripherally acting P-blocker (PABRA).
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Paragraph 00299; 00300
(2020/10/18)
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- HETEROARYL OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to heteroaryl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 38; 39
(2016/07/05)
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- Efficient enhancement of copper-pyridineoxazoline catalysts through immobilization and process design
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Copper-pyridineoxazoline (Cu-pyox) complexes are poor homogeneous catalysts for asymmetric cyclopropanation reactions. Pyox ligands have been immobilized by polymerization of monomers possessing a vinyl group directly attached to position 6 with styrene a
- Aranda,Cornejo,Fraile,Garcia-Verdugo,Gil,Luis,Mayoral,Martinez-Merino,Ochoa
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p. 983 - 990
(2011/06/19)
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- Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists
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A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives was synthesized, and their structure-activity relationships were examined in order to identify potent and selective arginine vasopressin V2 receptor agonists. Attempts to substitute other chemical groups in place of the 2-pyridilmethyl moiety of 1a led to the discovery that potent V2 binding affinity could be obtained with a wide range of functional groups. This structural tolerance allowed for the manipulation of other attributes, such as selectivity against V1a receptor affinity or avoidance of the undesirable inhibition of cytochrome P450 (CYP), without losing potent affinity for the V2 receptor. Some representative compounds obtained in this study were also found to decrease urine volume in awake rats.
- Tsukamoto, Issei,Koshio, Hiroyuki,Kuramochi, Takahiro,Saitoh, Chikashi,Yanai-Inamura, Hiroko,Kitada-Nozawa, Chika,Yamamoto, Eisaku,Yatsu, Takeyuki,Shimada, Yoshiaki,Sakamoto, Shuichi,Tsukamoto, Shin-ichi
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experimental part
p. 3130 - 3141
(2009/09/30)
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